Abstract
Objective(s):
The aim of this work was to prepare and characterize magnetic nanoparticles (MNPs) as theranostic system to act simultaneously as drug carrier and MRI contrast agent. Chitosan-coated MNPs (CMNPs) were prepared and loaded with silymarin. Silymarin-loaded CMNPs were characterized with various techniques and their potential as MRI contrast agent was also evaluated.
Materials and Methods:
The chitosan-coated MNPs were prepared by coprecipitation method and were loaded with silymarin. The synthesized nanoparticles were characterized by various techniques including SEM, TEM, X‐ray diffraction (XRD), FTIR and vibrating sample magnetometer (VSM). In vitro drug release of silymarin was evaluated at 37 ˚C at pH 5.3 and 7.4. Then, their proton relaxivity was evaluated to study the potential of CMNPs as MRI contrast agent in terms of r1 and r2.
Results:
Silymarin-loaded CMNPs were successfully prepared and characterized by FTIR and XRD techniques. VSM analysis revealed superparamagnetic properties of CMNPs. The release study showed that the maximum drug release accessible for CMNPs in pH=5.3 was higher than pH=7.4. Finally, the r2/r1 value of CMNPs was found to be close to 20 indicating that CMNPs has a strong efficiency as T2 contrast agents for MRI imaging.
Conclusion:
The findings demonstrated the potential of CMNPs as efficient MRI contrast agent as well as silymarin drug delivery.
This document describes the development and validation of a stability-indicating high-performance thin layer chromatography (HPTLC) method for the analysis of modafinil, both as a bulk drug and in tablet formulations. The method utilizes silica gel plates with an ethyl acetate, acetone and methanol mobile phase. Modafinil demonstrates good linearity, precision, accuracy and robustness within the method validation parameters. The method is also shown to distinguish modafinil from its degradation products formed under various stress conditions like acid and base hydrolysis, oxidation, photolysis and heat. The developed HPTLC method can be applied for the quantitative analysis and identification of modafinil in pharmaceutical formulations.
Preparation and characterization of poly (2 hydroxyethyl methacrylate) (phema...Alexander Decker
This document discusses the preparation and characterization of poly(2-hydroxyethyl methacrylate) (PHEMA) nanoparticles for potential use in controlled drug delivery. PHEMA nanoparticles were prepared using a modified suspension polymerization technique. The nanoparticles were characterized using infrared spectroscopy, scanning electron microscopy, and particle size analysis. The nanoparticles were found to be less than 100 nm in size and spherical or elliptical in shape, making them suitable for biomedical applications such as controlled drug delivery.
IOSR Journal of Pharmacy (IOSRPHR), www.iosrphr.org, call for paper, research...iosrphr_editor
This document discusses lectin-mediated drug delivery and therapeutics. It begins by introducing the concept of using lectins to specifically target drug delivery systems to sites via direct or reverse targeting based on unique carbohydrate moieties. It then discusses different approaches to lectin-based drug targeting including using prodrugs and conjugating drugs to lectins. Specific examples of lectins that have potential for cancer therapy are also provided. The document concludes by briefly mentioning the use of carbohydrates in vaccines and anti-adhesion therapeutics.
The Radiosensitivity Effect of Hydroxyurea on HT29 Cell Lineiosrphr_editor
The IOSR Journal of Pharmacy (IOSRPHR) is an open access online & offline peer reviewed international journal, which publishes innovative research papers, reviews, mini-reviews, short communications and notes dealing with Pharmaceutical Sciences( Pharmaceutical Technology, Pharmaceutics, Biopharmaceutics, Pharmacokinetics, Pharmaceutical/Medicinal Chemistry, Computational Chemistry and Molecular Drug Design, Pharmacognosy & Phytochemistry, Pharmacology, Pharmaceutical Analysis, Pharmacy Practice, Clinical and Hospital Pharmacy, Cell Biology, Genomics and Proteomics, Pharmacogenomics, Bioinformatics and Biotechnology of Pharmaceutical Interest........more details on Aim & Scope).
Simultaneous loading of 5-florouracil and SPIONs in HSA nanoparticles: Optimi...Nanomedicine Journal (NMJ)
Objective(s): Over the past two decades, considerable interest has been focused on utilizing biocompatible magnetic nanoparticles (MNPs) for biomedical applications. In this study, production of human serum albumin (HSA) nanoparticles using desolvation technique that were simultaneous loaded with high amounts of superparamagnetic iron oxide nanoparticles (SPIONs) and 5-flourouracil (5-FU) was investigated.
Materials and Methods: 5-FU loading (%) and SPIONs entrapment efficiency (%) were optimized using response surface methodology (RSM). The design expert software used to analyse the interactive effects of pH, 5-FU and SPIONs concentrations.
Results:The optimum conditions found to be pH of 8.2, drug concentration of 1.5 mg/ml and SPIONs concentration of 2.79 mg/ml. Under the mentioned optimum conditions, particles with the size of 111.8 nm, zeta potential of -37.1 mV, 5-FU loading of 15.8% and SPIONs entrapment efficiency of 41.1% were obtained. In vitro cumulative release of 5-FU from the nanoparticles was evaluated in phosphate buffer saline (pH 7.4, 37 °C). Results indicated that 85% of the 5-FU released during 95 h, which revealed a sustained release profile. In addition, Vibrating Sample Magnetometer (VSM) analyses confirmed the superparamagnetic properties of magnetic albumin nanoparticles manufactured under the optimum conditions.
Conclusion: According to the findings,SPIONs and 5-FU loaded HAS nanoparticles arepromising for use as novel targeted delivery system due to proper magnetic and drug release behaviours.
MAGNETICALLY MODULATED DRUG DELIVERY SYSTEMSSarangDalvi
This document discusses magnetic drug targeting, which uses magnetic fields to specifically deliver therapeutic agents to target areas of the body. Magnetic particles are bound to or encapsulate drugs and are injected, then an external magnetic field guides them to the target site. This allows high drug concentrations at the target with lower systemic exposure. Advantages include reduced side effects and doses needed. Magnetic carriers discussed include microspheres, liposomes, and nanoparticles. Applications include tumor targeting with chemotherapy or radiotherapy. Further research is still needed on magnetic properties, particle safety, and characterization to improve this targeted drug delivery approach.
Magnetically Modulated drug delivery system, Noval Drug Delivery system, New approaches to develop magnetically modulated drug delivery system and Formulation Design.
Formulation and Evaluation of Intranasal Microemulsion containing RutinSagar Savale
Rutin-flavonoid-polyphenolic has gained attention in prevention of brain cancer. The low
permeability of Rutin (RU) across the blood-brain-barrier (BBB) leads to its insufficient delivery which in
turns result in low therapeutic index. Therefore, developing a novel approaches enhancing the CNS delivery
of RU are required for the treatment of Cancer. The aim of this research work was to develop in
Microemulsion (ME) loaded with RU, for CNS targeting
This document describes the development and validation of a stability-indicating high-performance thin layer chromatography (HPTLC) method for the analysis of modafinil, both as a bulk drug and in tablet formulations. The method utilizes silica gel plates with an ethyl acetate, acetone and methanol mobile phase. Modafinil demonstrates good linearity, precision, accuracy and robustness within the method validation parameters. The method is also shown to distinguish modafinil from its degradation products formed under various stress conditions like acid and base hydrolysis, oxidation, photolysis and heat. The developed HPTLC method can be applied for the quantitative analysis and identification of modafinil in pharmaceutical formulations.
Preparation and characterization of poly (2 hydroxyethyl methacrylate) (phema...Alexander Decker
This document discusses the preparation and characterization of poly(2-hydroxyethyl methacrylate) (PHEMA) nanoparticles for potential use in controlled drug delivery. PHEMA nanoparticles were prepared using a modified suspension polymerization technique. The nanoparticles were characterized using infrared spectroscopy, scanning electron microscopy, and particle size analysis. The nanoparticles were found to be less than 100 nm in size and spherical or elliptical in shape, making them suitable for biomedical applications such as controlled drug delivery.
IOSR Journal of Pharmacy (IOSRPHR), www.iosrphr.org, call for paper, research...iosrphr_editor
This document discusses lectin-mediated drug delivery and therapeutics. It begins by introducing the concept of using lectins to specifically target drug delivery systems to sites via direct or reverse targeting based on unique carbohydrate moieties. It then discusses different approaches to lectin-based drug targeting including using prodrugs and conjugating drugs to lectins. Specific examples of lectins that have potential for cancer therapy are also provided. The document concludes by briefly mentioning the use of carbohydrates in vaccines and anti-adhesion therapeutics.
The Radiosensitivity Effect of Hydroxyurea on HT29 Cell Lineiosrphr_editor
The IOSR Journal of Pharmacy (IOSRPHR) is an open access online & offline peer reviewed international journal, which publishes innovative research papers, reviews, mini-reviews, short communications and notes dealing with Pharmaceutical Sciences( Pharmaceutical Technology, Pharmaceutics, Biopharmaceutics, Pharmacokinetics, Pharmaceutical/Medicinal Chemistry, Computational Chemistry and Molecular Drug Design, Pharmacognosy & Phytochemistry, Pharmacology, Pharmaceutical Analysis, Pharmacy Practice, Clinical and Hospital Pharmacy, Cell Biology, Genomics and Proteomics, Pharmacogenomics, Bioinformatics and Biotechnology of Pharmaceutical Interest........more details on Aim & Scope).
Simultaneous loading of 5-florouracil and SPIONs in HSA nanoparticles: Optimi...Nanomedicine Journal (NMJ)
Objective(s): Over the past two decades, considerable interest has been focused on utilizing biocompatible magnetic nanoparticles (MNPs) for biomedical applications. In this study, production of human serum albumin (HSA) nanoparticles using desolvation technique that were simultaneous loaded with high amounts of superparamagnetic iron oxide nanoparticles (SPIONs) and 5-flourouracil (5-FU) was investigated.
Materials and Methods: 5-FU loading (%) and SPIONs entrapment efficiency (%) were optimized using response surface methodology (RSM). The design expert software used to analyse the interactive effects of pH, 5-FU and SPIONs concentrations.
Results:The optimum conditions found to be pH of 8.2, drug concentration of 1.5 mg/ml and SPIONs concentration of 2.79 mg/ml. Under the mentioned optimum conditions, particles with the size of 111.8 nm, zeta potential of -37.1 mV, 5-FU loading of 15.8% and SPIONs entrapment efficiency of 41.1% were obtained. In vitro cumulative release of 5-FU from the nanoparticles was evaluated in phosphate buffer saline (pH 7.4, 37 °C). Results indicated that 85% of the 5-FU released during 95 h, which revealed a sustained release profile. In addition, Vibrating Sample Magnetometer (VSM) analyses confirmed the superparamagnetic properties of magnetic albumin nanoparticles manufactured under the optimum conditions.
Conclusion: According to the findings,SPIONs and 5-FU loaded HAS nanoparticles arepromising for use as novel targeted delivery system due to proper magnetic and drug release behaviours.
MAGNETICALLY MODULATED DRUG DELIVERY SYSTEMSSarangDalvi
This document discusses magnetic drug targeting, which uses magnetic fields to specifically deliver therapeutic agents to target areas of the body. Magnetic particles are bound to or encapsulate drugs and are injected, then an external magnetic field guides them to the target site. This allows high drug concentrations at the target with lower systemic exposure. Advantages include reduced side effects and doses needed. Magnetic carriers discussed include microspheres, liposomes, and nanoparticles. Applications include tumor targeting with chemotherapy or radiotherapy. Further research is still needed on magnetic properties, particle safety, and characterization to improve this targeted drug delivery approach.
Magnetically Modulated drug delivery system, Noval Drug Delivery system, New approaches to develop magnetically modulated drug delivery system and Formulation Design.
Formulation and Evaluation of Intranasal Microemulsion containing RutinSagar Savale
Rutin-flavonoid-polyphenolic has gained attention in prevention of brain cancer. The low
permeability of Rutin (RU) across the blood-brain-barrier (BBB) leads to its insufficient delivery which in
turns result in low therapeutic index. Therefore, developing a novel approaches enhancing the CNS delivery
of RU are required for the treatment of Cancer. The aim of this research work was to develop in
Microemulsion (ME) loaded with RU, for CNS targeting
LC-MS compatible stability indicating RP-UPLC method for the estimation of es...Ratnakaram Venkata Nadh
58. G. Venkata Narasimha Rao, Muralee Krishna, Ravi Kumar Bellam and R. Venkata Nadh, LC-MS compatible stability indicating RP-UPLC method for the estimation of ester prodrug of mycophenolic acid in injection formulation, Asian Journal of Chemistry, (SCOPUS indexed, ISSN: 0970-7077 (Print), 0975-427X (Online)), 30(8) (2018) 1915-1924, DOI: 10.14233/ajchem.2018.21445
This document discusses the use of nanoparticles in drug delivery systems. Nanoparticles can be used to more precisely control the release of drugs in the body over time compared to traditional drug dosing. Magnetic nanoparticles are particularly useful as they can be guided to specific target sites in the body using external magnetic fields. The document outlines various methods for synthesizing magnetic nanoparticles and functionalizing them for drug delivery applications. Characterization techniques are also discussed for analyzing the nanoparticles. The document concludes that magnetic nanoparticles have the potential to improve drug targeting and control drug release while maintaining low toxicity.
Ion-pair Formation for the Determination of Mianserin Using Fast Sulphon Black FRatnakaram Venkata Nadh
This document presents a method for the colorimetric determination of the antidepressant drug mianserin using Fast Sulphon Black F (FSBF) dye. Reaction conditions were optimized to form a soluble colored ion-pair complex between the protonated form of mianserin and the anionic form of FSBF in dichloromethane. The method was validated according to ICH guidelines and showed good linearity, accuracy, precision and recovery for mianserin quantification. The developed method was successfully applied to determine mianserin levels in tablet formulations.
Magnetic microspheres are small particles containing magnetite that can be guided to target tissues using external magnetic fields. They allow drugs to be delivered at lower doses directly to tissues while avoiding toxicity. Microspheres are prepared using methods like phase separation or solvent evaporation to encapsulate drugs and magnetite in carriers like albumin. Particle characteristics and drug release kinetics can be evaluated using techniques like dialysis, imaging, and microscopy. Magnetic microspheres show potential for targeted drug delivery but also have technical challenges for approval.
This document discusses nanoparticles as drug delivery systems. It begins with definitions and concepts, describing nanoparticles as subnanosized colloidal systems ranging from 10-1000 nm that can be used to selectively deliver drugs to target tissues. It then covers the advantages and disadvantages of nanoparticles, ideal characteristics, methods of preparation including cross-linking and polymerization, characterization techniques, applications such as cancer therapy and DNA delivery, and concludes with references.
This document discusses various NMR techniques for ligand screening in drug discovery. It begins by providing background on the increasing role of NMR in drug research due to its ability to sensitively detect molecular interactions and provide structural information. The document then reviews both ligand-observed and target-observed NMR screening techniques, describing methods based on changes in molecular diffusion, relaxation, and intramolecular or intermolecular magnetization transfer upon ligand binding. Specific techniques discussed include saturation transfer difference (STD) NMR, transferred nuclear Overhauser effect (trNOE), and NOE pumping. The review concludes by noting the dual importance of NMR for drug screening and structure-based drug design.
This document describes two spectrophotometric methods (Methods A and B) developed for the quantification of etoricoxib (ETX) in tablets. Method A is an area under curve method using integrated absorbance values between 215-244nm. Method B is a first derivative spectroscopy method measuring amplitude at 236nm. Both methods showed linearity between 2-16μg/ml of ETX. The proposed methods were validated and found to accurately quantify ETX in tablets without interference from excipients, as determined through assay and recovery experiments. The methods were concluded to be simple, sensitive, accurate and useful for routine analysis of ETX in pharmaceutical formulations.
The document summarizes a presentation on nanoparticles. It begins with an introduction defining nanoparticles as particulate dispersions between 10-1000nm in size. It then discusses the ideal properties of nanoparticles for drug delivery including stability and non-toxicity. Some advantages are increased therapeutic efficacy and targeted drug delivery. Potential disadvantages include limited targeting abilities and toxicity. Different types of nanoparticles are described such as nanocapsules, nanospheres, solid lipid nanoparticles and polymeric nanoparticles. Methods of preparation include polymerization, ionic gelation and use of preformed polymers. Evaluation methods are also summarized such as assessing particle size, drug content and in vitro drug release.
This document provides an overview of basic concepts in biopharmaceutics including pharmacokinetic models and parameters. It discusses pharmacokinetic concepts like dosage regimen, pharmacokinetics, plasma drug concentration profiles, and pharmacokinetic parameters including Cmax, tmax, AUC, etc. It also covers pharmacokinetic models including compartment models, physiological models, and non-compartmental analysis. Specific compartment models like one-compartment open model for IV bolus and infusion administrations as well as extravascular administration are explained. Methods for estimating pharmacokinetic parameters from these models are also summarized.
This document describes a two-step method for immobilizing targeting molecules onto buckminsterfullerenes (C60) for drug delivery applications. The method uses 1-pyrenebutanoic acid, succinimidyl ester (PASE) to noncovalently attach to C60 via π-stacking interactions. PASE then forms covalent amide bonds with amine groups on targeting molecules like the aptamer AS1411. Infrared spectroscopy confirmed the successful immobilization of AS1411 onto C60 through the absence of characteristic NHS peaks and presence of peaks corresponding to C60, PASE and the aptamer's phosphate groups. This simple two-step method allows a wide range of targeting molecules
This document discusses using star-shaped carboxy-terminated polylactide (SSPLA) grafted onto chitosan (CS) to create nanoparticles for controlled drug release. The nanoparticles were prepared using polyelectrolyte complexation of CS-SSPLA and dextran sulfate, and encapsulated doxorubicin with over 80% efficiency. Release studies showed the SSPLA reduced the initial burst release by up to 100% compared to CS nanoparticles alone. The CS-SSPLA nanoparticles provided a lag time of 1-3 hours before sustained release, indicating their potential for controlled drug delivery applications.
This document discusses mucosal drug delivery systems, outlining their anatomy and physiology, permeation methods, permeability enhancers, buccal and sublingual delivery systems, and evaluation techniques. Specific routes mentioned include oral mucosa delivery via the buccal and sublingual areas. Permeation occurs through both trans and para cellular pathways, and various enhancers can improve permeability. Both in vivo and in vitro tests are used to evaluate these mucosal delivery systems.
“Microparticles are defined as particulate dispersions or solid particles with a size in the range of 1-1000 μm.”
The drug is dissolved, entrapped, encapsulated or attached to a microparticle matrix.
This document provides an overview of targeted drug delivery systems. It begins with definitions of targeted drug delivery as selectively delivering medication to its site of action to increase concentration there relative to other tissues. The document then discusses the concept and rational for targeted delivery, ideal characteristics, advantages, disadvantages, and various strategies and types of targeted systems. These include passive targeting utilizing the body's natural biodistribution, active targeting using functionalized carriers, and types of carriers like liposomes, dendrimers, nanotubes, and nanocrystals.
1) The document describes a study on using mesoporous metal-organic frameworks (MOFs) as nanocarriers for controlled drug release in chemotherapy. Zirconium-based MOF nanoparticles were synthesized to carry and release doxorubicin and cisplatin.
2) The MOF nanoparticles were found to have high drug loading capacity and provided controlled release of the chemotherapeutic drugs through their porous structure. In vitro tests showed the drugs were effectively released and reduced cancer cell viability.
3) The results suggest mesoporous MOFs have potential as nanocarriers for chemotherapy by improving drug pharmacokinetics and maximizing effectiveness through controlled release at tumor sites.
This document discusses targeted drug delivery systems. It begins with an introduction defining targeted drug delivery as selectively delivering medication only to its site of action and not other organs. It then discusses various strategies for targeted delivery including passive targeting using physiological properties and active targeting using surface modifications like antibodies. Several types of targeted delivery systems are mentioned, such as liposomes, nanotubes, nanoshells and others, along with their applications. The advantages of targeted delivery in reducing toxicity and dose are also outlined.
The document discusses drug delivery systems and targeted drug delivery. It begins by providing market size information for current drug delivery systems and definitions of key terms like prolonged release, zero-order release, and bio-responsive release. It then covers classifications of targeted drug delivery systems based on mechanism, including passive targeting, active targeting, and dual targeting. Different carrier systems, dosages forms, and specific applications for brain and cancer targeting are discussed in detail.
This document discusses solid lipid nanoparticles (SLNs), which are a promising drug delivery system. SLNs consist of nanoparticles made of physiological lipids that can incorporate both hydrophilic and hydrophobic drugs. The document outlines several preparation methods for SLNs, including high pressure homogenization and ultrasonication. It also discusses the advantages of SLNs, such as their small size, high drug loading capacity, and avoidance of organic solvents, as well as some limitations. Overall, the document presents an overview of SLNs for use as a versatile drug delivery system.
Abstract
Objective(s):
The development of reliable and ecofriendly process for the synthesis of nano-metals is an important aspect in the field of nanotechnology. Nano-metals are a special group of materials with broad area of applications.
Materials and Methods:
In this study, extracellular synthesis of silver nanoparticles (SNPs) performed by use of the gram positive soil Streptomycetes. Streptomycetes isolated from rice fields of Guilan Province, Iran (5 isolates). Initial characterization of SNPs was performed by visual change color. To determine the bacterium taxonomical identity, its colonies characterized morphologically by use of scanning electron microscope. The PCR molecular analysis of active isolate represented its identity partially. In this regard, 16S rDNA of isolate G was amplified using universal bacterial primers FD1 and RP2. The PCR products were purified and sequenced. Sequence analysis of 16S rDNA was then conducted using NCBI GenBank database using BLAST. Also SNPs were characterized by, transmission electron microscopy (TEM) and X-ray diffraction spectroscopy (XRD).
Results:
From all 5 collected Streptomyces somaliensis isolates, isolate G showed highest extracellular synthesis of SNPs via in vitro. SNPs were formed immediately by the addition of (AgNO3) solution (1 mM). UV-visible spectrophotometry for measuring surface plasmon resonance showed a single absorption peak at 450 nm, which confirmed the presence of SNPs. TEM revealed the extracellular formation of spherical silver nanoparticles in the size range of 5-35 nm.
Conclusions:
The biological approach for the synthesis of metal nanoparticles offers an environmentally benign alternative to the traditional chemical and physical synthesis methods. So, a simple, environmentally friendly and cost-effective method has been developed to synthesize AgNPs using Streptomycetes.
LC-MS compatible stability indicating RP-UPLC method for the estimation of es...Ratnakaram Venkata Nadh
58. G. Venkata Narasimha Rao, Muralee Krishna, Ravi Kumar Bellam and R. Venkata Nadh, LC-MS compatible stability indicating RP-UPLC method for the estimation of ester prodrug of mycophenolic acid in injection formulation, Asian Journal of Chemistry, (SCOPUS indexed, ISSN: 0970-7077 (Print), 0975-427X (Online)), 30(8) (2018) 1915-1924, DOI: 10.14233/ajchem.2018.21445
This document discusses the use of nanoparticles in drug delivery systems. Nanoparticles can be used to more precisely control the release of drugs in the body over time compared to traditional drug dosing. Magnetic nanoparticles are particularly useful as they can be guided to specific target sites in the body using external magnetic fields. The document outlines various methods for synthesizing magnetic nanoparticles and functionalizing them for drug delivery applications. Characterization techniques are also discussed for analyzing the nanoparticles. The document concludes that magnetic nanoparticles have the potential to improve drug targeting and control drug release while maintaining low toxicity.
Ion-pair Formation for the Determination of Mianserin Using Fast Sulphon Black FRatnakaram Venkata Nadh
This document presents a method for the colorimetric determination of the antidepressant drug mianserin using Fast Sulphon Black F (FSBF) dye. Reaction conditions were optimized to form a soluble colored ion-pair complex between the protonated form of mianserin and the anionic form of FSBF in dichloromethane. The method was validated according to ICH guidelines and showed good linearity, accuracy, precision and recovery for mianserin quantification. The developed method was successfully applied to determine mianserin levels in tablet formulations.
Magnetic microspheres are small particles containing magnetite that can be guided to target tissues using external magnetic fields. They allow drugs to be delivered at lower doses directly to tissues while avoiding toxicity. Microspheres are prepared using methods like phase separation or solvent evaporation to encapsulate drugs and magnetite in carriers like albumin. Particle characteristics and drug release kinetics can be evaluated using techniques like dialysis, imaging, and microscopy. Magnetic microspheres show potential for targeted drug delivery but also have technical challenges for approval.
This document discusses nanoparticles as drug delivery systems. It begins with definitions and concepts, describing nanoparticles as subnanosized colloidal systems ranging from 10-1000 nm that can be used to selectively deliver drugs to target tissues. It then covers the advantages and disadvantages of nanoparticles, ideal characteristics, methods of preparation including cross-linking and polymerization, characterization techniques, applications such as cancer therapy and DNA delivery, and concludes with references.
This document discusses various NMR techniques for ligand screening in drug discovery. It begins by providing background on the increasing role of NMR in drug research due to its ability to sensitively detect molecular interactions and provide structural information. The document then reviews both ligand-observed and target-observed NMR screening techniques, describing methods based on changes in molecular diffusion, relaxation, and intramolecular or intermolecular magnetization transfer upon ligand binding. Specific techniques discussed include saturation transfer difference (STD) NMR, transferred nuclear Overhauser effect (trNOE), and NOE pumping. The review concludes by noting the dual importance of NMR for drug screening and structure-based drug design.
This document describes two spectrophotometric methods (Methods A and B) developed for the quantification of etoricoxib (ETX) in tablets. Method A is an area under curve method using integrated absorbance values between 215-244nm. Method B is a first derivative spectroscopy method measuring amplitude at 236nm. Both methods showed linearity between 2-16μg/ml of ETX. The proposed methods were validated and found to accurately quantify ETX in tablets without interference from excipients, as determined through assay and recovery experiments. The methods were concluded to be simple, sensitive, accurate and useful for routine analysis of ETX in pharmaceutical formulations.
The document summarizes a presentation on nanoparticles. It begins with an introduction defining nanoparticles as particulate dispersions between 10-1000nm in size. It then discusses the ideal properties of nanoparticles for drug delivery including stability and non-toxicity. Some advantages are increased therapeutic efficacy and targeted drug delivery. Potential disadvantages include limited targeting abilities and toxicity. Different types of nanoparticles are described such as nanocapsules, nanospheres, solid lipid nanoparticles and polymeric nanoparticles. Methods of preparation include polymerization, ionic gelation and use of preformed polymers. Evaluation methods are also summarized such as assessing particle size, drug content and in vitro drug release.
This document provides an overview of basic concepts in biopharmaceutics including pharmacokinetic models and parameters. It discusses pharmacokinetic concepts like dosage regimen, pharmacokinetics, plasma drug concentration profiles, and pharmacokinetic parameters including Cmax, tmax, AUC, etc. It also covers pharmacokinetic models including compartment models, physiological models, and non-compartmental analysis. Specific compartment models like one-compartment open model for IV bolus and infusion administrations as well as extravascular administration are explained. Methods for estimating pharmacokinetic parameters from these models are also summarized.
This document describes a two-step method for immobilizing targeting molecules onto buckminsterfullerenes (C60) for drug delivery applications. The method uses 1-pyrenebutanoic acid, succinimidyl ester (PASE) to noncovalently attach to C60 via π-stacking interactions. PASE then forms covalent amide bonds with amine groups on targeting molecules like the aptamer AS1411. Infrared spectroscopy confirmed the successful immobilization of AS1411 onto C60 through the absence of characteristic NHS peaks and presence of peaks corresponding to C60, PASE and the aptamer's phosphate groups. This simple two-step method allows a wide range of targeting molecules
This document discusses using star-shaped carboxy-terminated polylactide (SSPLA) grafted onto chitosan (CS) to create nanoparticles for controlled drug release. The nanoparticles were prepared using polyelectrolyte complexation of CS-SSPLA and dextran sulfate, and encapsulated doxorubicin with over 80% efficiency. Release studies showed the SSPLA reduced the initial burst release by up to 100% compared to CS nanoparticles alone. The CS-SSPLA nanoparticles provided a lag time of 1-3 hours before sustained release, indicating their potential for controlled drug delivery applications.
This document discusses mucosal drug delivery systems, outlining their anatomy and physiology, permeation methods, permeability enhancers, buccal and sublingual delivery systems, and evaluation techniques. Specific routes mentioned include oral mucosa delivery via the buccal and sublingual areas. Permeation occurs through both trans and para cellular pathways, and various enhancers can improve permeability. Both in vivo and in vitro tests are used to evaluate these mucosal delivery systems.
“Microparticles are defined as particulate dispersions or solid particles with a size in the range of 1-1000 μm.”
The drug is dissolved, entrapped, encapsulated or attached to a microparticle matrix.
This document provides an overview of targeted drug delivery systems. It begins with definitions of targeted drug delivery as selectively delivering medication to its site of action to increase concentration there relative to other tissues. The document then discusses the concept and rational for targeted delivery, ideal characteristics, advantages, disadvantages, and various strategies and types of targeted systems. These include passive targeting utilizing the body's natural biodistribution, active targeting using functionalized carriers, and types of carriers like liposomes, dendrimers, nanotubes, and nanocrystals.
1) The document describes a study on using mesoporous metal-organic frameworks (MOFs) as nanocarriers for controlled drug release in chemotherapy. Zirconium-based MOF nanoparticles were synthesized to carry and release doxorubicin and cisplatin.
2) The MOF nanoparticles were found to have high drug loading capacity and provided controlled release of the chemotherapeutic drugs through their porous structure. In vitro tests showed the drugs were effectively released and reduced cancer cell viability.
3) The results suggest mesoporous MOFs have potential as nanocarriers for chemotherapy by improving drug pharmacokinetics and maximizing effectiveness through controlled release at tumor sites.
This document discusses targeted drug delivery systems. It begins with an introduction defining targeted drug delivery as selectively delivering medication only to its site of action and not other organs. It then discusses various strategies for targeted delivery including passive targeting using physiological properties and active targeting using surface modifications like antibodies. Several types of targeted delivery systems are mentioned, such as liposomes, nanotubes, nanoshells and others, along with their applications. The advantages of targeted delivery in reducing toxicity and dose are also outlined.
The document discusses drug delivery systems and targeted drug delivery. It begins by providing market size information for current drug delivery systems and definitions of key terms like prolonged release, zero-order release, and bio-responsive release. It then covers classifications of targeted drug delivery systems based on mechanism, including passive targeting, active targeting, and dual targeting. Different carrier systems, dosages forms, and specific applications for brain and cancer targeting are discussed in detail.
This document discusses solid lipid nanoparticles (SLNs), which are a promising drug delivery system. SLNs consist of nanoparticles made of physiological lipids that can incorporate both hydrophilic and hydrophobic drugs. The document outlines several preparation methods for SLNs, including high pressure homogenization and ultrasonication. It also discusses the advantages of SLNs, such as their small size, high drug loading capacity, and avoidance of organic solvents, as well as some limitations. Overall, the document presents an overview of SLNs for use as a versatile drug delivery system.
Abstract
Objective(s):
The development of reliable and ecofriendly process for the synthesis of nano-metals is an important aspect in the field of nanotechnology. Nano-metals are a special group of materials with broad area of applications.
Materials and Methods:
In this study, extracellular synthesis of silver nanoparticles (SNPs) performed by use of the gram positive soil Streptomycetes. Streptomycetes isolated from rice fields of Guilan Province, Iran (5 isolates). Initial characterization of SNPs was performed by visual change color. To determine the bacterium taxonomical identity, its colonies characterized morphologically by use of scanning electron microscope. The PCR molecular analysis of active isolate represented its identity partially. In this regard, 16S rDNA of isolate G was amplified using universal bacterial primers FD1 and RP2. The PCR products were purified and sequenced. Sequence analysis of 16S rDNA was then conducted using NCBI GenBank database using BLAST. Also SNPs were characterized by, transmission electron microscopy (TEM) and X-ray diffraction spectroscopy (XRD).
Results:
From all 5 collected Streptomyces somaliensis isolates, isolate G showed highest extracellular synthesis of SNPs via in vitro. SNPs were formed immediately by the addition of (AgNO3) solution (1 mM). UV-visible spectrophotometry for measuring surface plasmon resonance showed a single absorption peak at 450 nm, which confirmed the presence of SNPs. TEM revealed the extracellular formation of spherical silver nanoparticles in the size range of 5-35 nm.
Conclusions:
The biological approach for the synthesis of metal nanoparticles offers an environmentally benign alternative to the traditional chemical and physical synthesis methods. So, a simple, environmentally friendly and cost-effective method has been developed to synthesize AgNPs using Streptomycetes.
The document discusses the passive voice in Spanish. It begins by distinguishing between the active voice, where the subject performs the action of the verb, and the passive voice, where the action of the verb is received by the object. It then provides instructions for transforming an active sentence into a passive sentence by making the object the subject and using the verb "to be" plus the past participle. Examples are given of active and corresponding passive sentences. Finally, it discusses how the verb changes form depending on its tense in the original active sentence and provides five more examples of sentences transformed from active to passive voice.
Polymeric composite membranes for temperature and pH-responsive delivery of d...Nanomedicine Journal (NMJ)
Abstract
Objective(s):
Nowadays hydrogels are one of the upcoming classes of polymer-based controlled-release drug delivery systems. Temperature and pH-responsive delivery systems have drawn much attention because some diseases reveal themselves by a change in temperature and/or pH. The objective of this work is to prepare and characterize composite membrane using responsive nanoparticles into a polymer matrix.
Materials and Methods:
These nanoparticles were made of the copolymer poly (N-isopropylacrylamide-co-methaçrylic acid) by an aqueous dispersion polymerization process and are responsible for dual sensitivity to temperature and pH. Morphology study with SEM, swelling behavior with Dynamic Light Scattering Technique, in vitro drug release behavior with side-by-side Diffusion Cells were also investigated in this paper. Doxorubicin hydrochloride was used as a model solute.
Results:
The study on the release of doxorubicin hydrochloride showed that the release rate was higher at pH 5 than pH 7.4, increased with the increase of temperature. Nevertheless, ionic strength only poses a minor direct effect at higher pH.
Conclusion:
Such system may be potentially used as a tumor-targeting doxorubicin hydrochloride delivery in the body.
Determination of acute toxicity and the effects of sub-acute concentrations o...Nanomedicine Journal (NMJ)
Abstract
Objective(s):
Copper oxidenanoparticles have different industrial applications so it is inevitable that nanoparticulate products finally find their way into aquatic ecosystems. Nevertheless there is little information available about their effects on some of edible fish. The present study aims to determine the acute toxicity and evaluate the effect of two sub-acute concentrations (50 and 70% 96 h LC50) of CuO-NPs on some hematological and biochemical parameters of R. rutilus.
Materials and Methods:
225 healthy specimen of R. rutilus (mean weight 5.52±1.2 g; mean length 6.20±0.2 cm) were transported to the laboratory. In order to prepare the stock solution, CuO-NPs was dispersed in pure water with ultrasonication (50-60 kHz) for 15 min every day before dosing. At first, R. rutilus was exposed to CuO-NPs to determine the lethal concentration (LC50) value. Following acute test, fish were treated with sub-acute concentrations of CuO-NPs (50 and 70% 96 h-LC50 at) with one control group (no CuO-NPs) for a week to determine the changes in the level of some plasma hematological and biochemical parameters.
Results:
The 96 h-LC50 values of CuO-NPs was 2.19±0.003 mg/l. R. rutilus exhibited significantly lower RBC count, Hb and Hct values and a significant increase in the WBC numbers, MCH, MCHC and MCV indices (p<0.05).><0.05).
Conclusion:
These alterations indicate R. rutilus sensitivity to CuO-NPs and changes in blood parameters would be a useful tool for measurement early exposure to CuO nanoparticles.
El resumen describe los resultados de una búsqueda en Scopus sobre el uso de acupuntura, masaje y técnicas de relajación para la depresión y ansiedad en personas de mediana edad. Se encontraron 384 documentos publicados desde 2005. El artículo más reciente se titula "The effect of upper-extremity aerobic exercise on complex regional pain syndrome type I: a randomized controlled study on subacute stroke". Fue escrito originalmente en inglés. El artículo más citado se titula "Survey of chronic pain in Europe: Prevalence, impact on daily life, and treatment" y tiene
The document provides summaries and box office information for 5 popular action movies: Fast & Furious 6, Avatar, Mission Impossible 3, Bad Boys 2, and Spider-Man 3. It summarizes the plots and includes each movie's budget, distributor, and worldwide box office earnings.
People spend a significant amount of time watching television and viewing commercials, though some commercials can be boring or repetitive. For a school project, students are tasked with creating their own 30-second television commercial, which involves planning the product or service, commercial style, script, filming techniques, and post-production editing within a 20-30 second time frame.
Este documento presenta un trabajo final realizado por Isaac Cruz Santisteban y presentado a María Alexandra León Martínez. El trabajo contiene varios temas sobre lectura, búsqueda de bibliografía e inferencia. El resumen concluye que la expresión oral y escrita sirve para definir situaciones de la vida diaria y enseña a tomar decisiones para desempeñarse como profesionales.
Spectrophotometric Estimation of Drugs Using Potassium Permanganate and Saffr...iosrjce
IOSR Journal of Applied Chemistry (IOSR-JAC) is a double blind peer reviewed International Journal that provides rapid publication (within a month) of articles in all areas of applied chemistry and its applications. The journal welcomes publications of high quality papers on theoretical developments and practical applications in Chemical Science. Original research papers, state-of-the-art reviews, and high quality technical notes are invited for publications.
Formulation and evaluation of oral biphasic drug delivery system of Metronida...inventionjournals
In the present study, a newly innovative drug delivery system of biphasic Metronidazole (MTZ) tablet has been studied. An attempt was made to improve the patient’s adherence and the potential clinical outcomes by reducing the dosing frequency by formulating bilayer tablets containing Metrodinazole. Each bilayer tablet is composed of a sustained release (SR) layer and an immediate release (IR) layer for rapid drug release. Five different formulations of bilayer tablets were formulated using HPMC as hydrophilic polymer to retarded the drug release and the effect of Starch and MCC on the release profile were evaluated. Wet granulation method was used to prepare granules of the immediate and sustained release layers. The tablets were evaluated for their physical parameters and all valuesobtained found to be within the acceptable limits. The dissolution test has been carried out using the USP type II rotating paddle. Collected samples were analyzed using the high performance liquid chromatography. The mechanisms of Metrodinazole release from the sustained release layer were fitted into zero-order, first order, Higuchi, Hixon- Crowell model and Korsmeyer-Peppas release model. The results of the dissolution profiles showed that the drug release from the sustained release layer varied depending on the amount of HPMC and the presence of Starch or MCC. The kinetics of the release of MTZ from the different formulations showed good fitting with Higuchi model with correlation coefficients (R2) of 0.9965 - 0.9985. From values obtained for the diffusional exponent, n, Korsmeyer-Peppas equation observed that for all the formulations n value ranged from 0.4662 to 0.5370, and this demonstrates that the release mechanism followed non-Fickian type of release ( anomalous transport).
Nanoparticle of plant extract: A Novel approach for cancer theraproshan telrandhe
Nanotechnology deals regulating matter at dimension of 1-100 nanometers. its use in fundamental physics, biology, chemistry, technology of nanometer scale objects. It also includes how such objects can be used in the areas of computation, sensors, nanostructure materials, biolabeling, biomedical, agricultural, biolabeling , cancer, biotechnology. There are 3 methods for preparation of nanoparticles Physical, chemical &biological. Cancer is as an abnormal growth of cells. It is due to lack of proper regulation in cell cycle. Cancer develops through an accumulation of genetic changes or mutations which could emerge due to different factors like physical, chemical, biological. Currently available cancer chemotherapeutic agents insidiously affect the host cells especially bone marrow, epithelial tissues, reticule-endothelial system and gonads Because of high death rate associated with cancer and the serious side effects of chemotherapy & radiation therapy. Silver NanoParticles as an anticancer agent and they have all turned up positive. Many plant-derived products have been reported to exhibit potent antitumour activity against several rodent and human cancer cell lines. Plants history about use in the treatment of cancer. It is significant that over 60% of currently used anticancer agents are derived, in one way or another, from natural sources (plants, marine organism, and microorganisms)
COMPLETE DESCRIPTION ABOUT DENDRIMERS ALONG THEIR ROLE IN CURRENT MEDICAL SYSTEM,THEIR USEAGE IN CHEMOTHERAPUTIC PURPOSES ETC IS PROVIDED IN THIS PRESENTATION.
This document summarizes research on developing a sustained release microencapsulated delivery system for the drug famotidine using a combination of mucoadhesive polymers. Famotidine microcapsules were prepared using an orifice ionic gelation technique with various polymer combinations, including carbopol-934 with hydroxypropyl methylcellulose, sodium carboxymethylcellulose, methylcellulose, or guar gum. The microcapsules were evaluated for properties like particle size, yield, drug entrapment efficiency, surface morphology, swelling properties, in vitro drug release, and mucoadhesion. The results showed that microcapsules prepared with sustained release polymers in combination exhibited slow release of famotidine over 9 hours with zero
The field of nanotechnology was first Discovered by Professor Richard P. Feynman in 1959 (Nobel laureate in physics, 1965) [2]. Nanotechnology is the science of the small; very small and it is used for the management of substance at a small scale. At this size, molecules and atoms work in a different way, and provide a variety of unpredicted and attractive uses .
PREPARATION AND CHARACTERIZATION OF POLY (Ɛ-CAPROLACTONE) NANOSUSPENSION CONT...VIJAY SINGH
This document summarizes the preparation and characterization of poly(Ɛ-caprolactone) nanosuspension containing the drug satranidazole. Satranidazole nanosuspensions were prepared using the nanoprecipitation method with poly(Ɛ-caprolactone) and sodium lauryl sulfate. The nanosuspensions were characterized in terms of particle size, zeta potential, drug entrapment efficiency, in vitro drug release, and stability. The optimized formulation of NS1a had a particle size of 241.6 nm, zeta potential of -21.3 mV, and drug entrapment efficiency of 72.61%. In vitro drug release studies showed higher release in simulated
Application of nanoparticals in drug delivery systemMalay Jivani
This document discusses nanoparticles and their applications in pharmaceuticals, with a focus on using gold nanoparticles (AuNPs) for cancer treatment. It defines nanoparticles and describes some common preparation methods. It then discusses several potential medical applications of nanoparticles, including using them as delivery systems for drugs, genes, and targeting cancer cells. Specifically for AuNPs, it covers their synthesis, properties, and how their surfaces can be functionalized. It describes how AuNPs may be useful for photothermal therapy, radiotherapy, and inhibiting angiogenesis for cancer treatment.
Formulation and in vitro evaluation of quercetin loaded carbon nanotubes for ...IRJET Journal
This document presents a study that formulated and evaluated quercetin-loaded carbon nanotubes for cancer targeting. Specifically, it:
1) Developed a quercetin-loaded drug delivery system using functionalized single-walled carbon nanotubes conjugated with chitosan.
2) Found that the highest drug loading efficiency of 38% was achieved at 4°C and with an equal initial weight ratio of drug to carrier.
3) Demonstrated that the drug delivery system was stable under neutral pH but effectively released quercetin under acidic pH similar to the tumor environment.
4) Showed that the quercetin-conjugated carrier had significantly higher cytotoxicity against HeLa
Nanoparticulate drug delivery system : recent advancesGayatriTiwaskar
Nanoparticulate drug-delivery systems (NPDDSs) are being explored for the purpose of solving the challenges of drug delivery. Most carriers are less than 100 nm in diameter and provide methods for targeting and releasing therapeutic compounds in defined regions.
These vehicles have the potential to eliminate or ameliorate many problems associated with drug distribution, precipitation at high concentrations, and toxicity issues with excipients. Many NPDDSs provide both hydrophobic and hydrophilic environments to facilitate drug solubility.
The document discusses various types of NPDDS like oral, pulmonary, topical, and parenteral systems. It also reviews formulation methods like emulsion, polymerization,
Polymeric Nanoparticles of Rifampicin were prepared by emulsion solvent evaporation technique using poly methyl methacrylate as polymer matrix and Poly vinyl alcohol as surfactant. Drug entrapped free flowing nanoparticles of Rifampicin were obtained after optimization using 32 factorial design and characterized for entrapment efficiency, particle size distribution, differential scanning calorimetry (DSC), X-ray diffraction (XRD), scanning electron microscopy (SEM) and in vitro and stability studies. The PMMA nanoparticles had a small size (213 ± 0.72 nm), uniform size distribution. The effects of dependent variables drug-polymer ratio and surfactant concentration on particle size and encapsulation efficiency were studied. The drug and polymer were not interacting with each other. SEM studies revealed the spherical shape of nanoparticles and in vitro release studies showed sustained drug release. RIF-polymeric nanoparticles drug delivery system proved to be promising for anti-tubercular therapy.
Nanoparticles ranging from 1 to 100 nanometers are being researched for targeted cancer treatment. They exhibit unique properties and are small enough to reach cancer cells. Researchers are working to develop nanoparticles that can selectively deliver drugs to kill cancer cells without harming healthy cells. The document reviews different preparation methods for nanoparticles, including solvent evaporation and ionic gelation. It also discusses evaluating nanoparticles based on size, stability, and in vitro drug release studies. Several FDA-approved nanoparticles are highlighted that use materials like liposomes, polymers, and albumin to encapsulate anticancer drugs. The potential applications of nanoparticles include improved drug delivery for cancer treatment and imaging.
This research article summarizes a study encapsulating curcumin, a natural anti-cancer compound, in polymeric micelles for cancer therapy. The researchers synthesized a diblock copolymer micelle (PNPC) from methoxy polyethylene glycol and oleic acid to encapsulate curcumin. They showed that PNPC had high drug loading efficiency and stability. In vitro, PNPC significantly suppressed the proliferation of breast and liver cancer cell lines. In an animal model of breast cancer, PNPC treatment reduced tumor incidence and size compared to controls. PNPC also increased expression of pro-apoptotic genes and decreased expression of anti-apoptotic and proliferative genes in the tumors. The results suggest PNPC is a
In vivo evaluation of mucoadhesive properties of nanoliposomal formulations u...Nanomedicine Journal (NMJ)
Objective(s):
Drug delivery via mucosal routes has been confirmed to be effective in inducing strong immune responses. Liposomes could enhance immune responses and mucoadhesive potentials, make them useful mucosal drug delivery systems. Coating of liposomes by mucoadhesive polymers succeeded in enhancing immune responses. Our studies aim at preparation and characterization of trimethylchitosan-coated nanoliposomes for nasal delivery of a model antigen, tetanus toxoid (TT).
Materials and Methods:
Anionic liposomes were prepared by dehydration-rehydration method with an average size of 100 nm and were coated with 0.01% (w/v) solution of trimethyulchitosan (TMC) with 50±10% of quaternization. Surface properties and zeta potential were evaluated by DLS. Antigen stability and integrity were studied by SDS-PAGE electrophoresis. Nasal clearance rate and mucoadhesive properties of liposomes were studied by gamma scintigraphy method using 99mTc-labelled liposomes.
Results:
The zeta potential of non-coated and TMC-coated liposomes was -40 and +38.8, respectively. Encapsulation rate of tetanus toxoid was 77 ± 5.5%. SDS-PAGE revealed that the antigens remained intact during formulation procedure. Gamma scintigraphy confirmed that both types of liposomes could remain in nasal cavity up to ten folds over the normal residence time for conventional nasal formulations.
Conclusion:
TMC-coated nanoliposomes have several positive potentials including good mucoadhesive properties, preserved integrity of loaded antigen and presence of TMC as a mucoadhesive polymer with innate immunoadjuvant potential which make them suitable for efficient adjuvant/delivery system.
Guar gum nanoparticles are smaller than 10-1000 nanometers and have properties distinct from larger particles. They can be prepared using ionic gelation and cross-linking methods. Dynamic light scattering, UV-Vis spectroscopy, and scanning electron microscopy are used to characterize the particles' size, morphology, and stability. Guar gum nanoparticles between 10-280 nm were successfully synthesized using these methods and characterized using these techniques. The particle size decreases with decreasing concentrations of guar gum and cross-linker. These nanoparticles have potential applications for targeted drug delivery.
This systematic review and meta-analysis examines the prognostic significance of microRNAs (miRNAs) in melanoma patients. Twenty-four studies across eight countries involving 2,669 melanoma patients were included. Sixteen studies reporting on the association between 25 miRNA expression levels and patient survival outcomes were eligible for meta-analysis. The pooled hazard ratio for up- and downregulated miRNA expression was 1.043, indicating a 4.3% increased likelihood of death. Subgroup analysis found miRNA10b, miRNA16 and miRNA21 expressions correlated with poor prognosis. The review aims to determine the prognostic roles and mean effect sizes of miRNAs to help predict patient outcomes and guide clinical decision making.
A nanocarrier is nano material being used as a transport module for another substance, such as a drug. Commonly used nanocarriers include micelles, polymers, carbon-based materials, liposomes and other substances.Nanocarriers are currently used in drug delivery and their unique characteristics demonstrate potential use in chemotherapy. Nanocarriers include polymer conjugates, polymeric nanoparticles, lipid-based carriers, dendrimers, carbon nanotubes, and gold Nanoparticles.Lipid-based carriers include both liposomes and micelles.
Examples of gold nanoparticles are gold nanoshells and nanocages.Different types of nonmaterial being used in nano carriers allows for hydrophobic and hydrophilic drugs to be delivered throughout the body.
potential problem with nanocarriers is unwanted toxicity from the type of nonmaterial being used. Inorganic nonmaterial can also be toxic to the human body if it accumulates in certain cell organelles new research is being conducted to invent more effective, safer nanocarriers.
Nano pharmaceuticals offer the ability to detect diseases at much earlier stages and the diagnostic applications could build upon conventional procedures using nano particles.
Nano pharmaceuticals represent an emerging field where the sizes of the drug particle or a therapeutic delivery system work at the nanoscale.
Nano pharmaceuticals have enormous potential in addressing this failure of traditional therapeutics which offers site-specific targeting of active agents.
Magnetic nanoparticles, bound to a suitable antibody, are used to label specific molecules, structures or microorganisms.
Gold nanoparticles tagged with short segments of DNA can be used for detection of genetic sequence in a sample.
Multicolor optical coding for biological assays has been achieved by embedding different-sized quantum dots into polymeric microbeads.
Nan pore technology for analysis of nucleic acids converts strings of nucleotides directly into electronic signatures.C-dots (Cornell dots) are the smallest silica-based nanoparticles with the size <10 nm.
There are three main reasons for the popularity of herbal medicine
1. There is a growing concern over the reliance and safety of drugs.
2. Modern medicine is failing to effectively treat many of the most common health condition.
3. Many natural measures are being shown to produce better results than drugs or surgery without the side effects
FORMULATION AND EVALUATION OF GELATIN MICROSPHERES LOADED WITH FENOFIBRATEReshma Fathima .K
The document summarizes the formulation and evaluation of gelatin microspheres loaded with the drug Fenofibrate. Two microsphere formulations were developed using a coacervation and phase separation method. Formulation F2 showed 97% drug encapsulation efficiency and released the drug over 12 hours, indicating it was suitable for oral sustained release. Evaluation tests on the microspheres showed they were spherical in shape, had good flow properties, and released the drug in a controlled manner without any burst release. The microspheres could facilitate the design of hard gelatin capsules for improved patient compliance.
Formulation and evaluation of gelatin microspheres loaded with fenofibrateVimal Patel
The document summarizes a study that formulated and evaluated gelatin microspheres loaded with the drug fenofibrate using a coacervation and phase separation method. Two microsphere formulations were developed with different drug to polymer ratios and evaluated for properties such as particle size, encapsulation efficiency, in vitro drug release, and stability. The results showed the microspheres had particle sizes between 5-10μm and encapsulation efficiencies between 70-97%. In vitro drug release studies found one formulation released the drug over 12 hours in a sustained manner. The study concluded this formulation was suitable for oral sustained release of fenofibrate.
Similar to Simultaneous diagnosis and drug delivery by silymarin-loaded magnetic nanoparticles (20)
Evaluation of the effect of crocetin on antitumor activity of doxorubicin enc...Nanomedicine Journal (NMJ)
Objective(s): The current study reports investigation of codelivery by PLGA nanoparticles (NPs) loaded with crocetin (Cro), a natural carotenoid dicarboxylicHYPERLINK “http://en.wikipedia.org/wiki/Carboxylic_acid” acid that is found in the crocus flower, and Doxorubicin (DOX).
Materials and Methods: Double emulsion/solvent evaporation method was used for preparation of PLGA nanoparticles containing Dox and Cro. Characterizations of prepared NPs were investigated by atomic force microscopy (AFM) and dynamic light scattering analysis. In vitro Cytotoxicity of DOX and Cro loaded PLGA NPs (PLGA-DOX-Cro) on MCF-7 cell line was evaluated using MTT test. Flow cytometry experiments were implemented to distinguish cells undergoing apoptosis from those undergoing necrosis. Furthermore the expression of caspase 3 was examined by western blot analysis.
Results: The prepared formulations had size of 150- 300 nm. Furthermore, PLGA-DOX-Cro nanoparticles inhibited MCF-7 tumor cells growth more efficiently than either DOX or Cro alone at the same concentrations, as quantified by MTT assay and flow cytometry. Studies on cellular uptake of DOX-Cro-NPs demonstrated that NPs were effectively taken up by MCF-7 tumor cells.
Conclusion: This study suggested that DOX-Cro-NPs may have promising applications in breast cancer therapy.
This study investigated codelivery of doxorubicin (DOX) and crocetin encapsulated in PLGA nanoparticles to treat breast cancer. PLGA nanoparticles containing both DOX and crocetin (PLGA-DOX-Cro NPs) were prepared using a double emulsion/solvent evaporation method. Characterization of the nanoparticles found them to be 150-300 nm in size. In vitro studies on MCF-7 breast cancer cells showed that PLGA-DOX-Cro NPs inhibited cell growth more than DOX or crocetin alone, as measured by MTT assay and flow cytometry. Cellular uptake studies also demonstrated effective uptake of the DOX-Cro-loaded NPs by MCF
Effects of combination of magnesium and zinc oxide nanoparticles and heat on ...Nanomedicine Journal (NMJ)
Objective: The objective of this study was to investigate the antibacterial activities of combination of MgO and ZnO nanoparticles in the presence of heat against Escherichia coli and Staphylococcus aureus.
Materials and Methods:Bacteria were grown on either agar or broth media followed by the addition of ZnO and MgO nanoparticles. Then the combined effect of ZnO and MgO nanoparticles was investigated. Furthermore, the media containing nanoparticles were treated with mild heat and their synergistic antibacterial activity was investigated against E. coli and S. aureus in milk.
Results: The data showed that the nanoparticles used in this study had no effect on the bacteria in the agar medium. However, the results showed that ZnO and MgO nanoparticles resulted in a significant decrease in the number of E. coli (P<0.000) and S. aureus (Pd”0.05) in the broth medium. The combination of nanoparticles and mild heat exhibited a significant decrease in the number of E. coli and S. aureus indicating the synergistic effects of nanoparticles and heat.
Conclusion: Using a combination of mild heat, ZnO and MgO nanoparticles, E. coli and S. aureus can be controlled successfully in the milk. Mild heating plus ZnO and MgO nanoparticles has a synergistic effect which would reduce the need for high temperature and also the concentrations of ZnO and MgO nanoparticles required for pathogen control in minimally processed milk during maintaining.
Preparation and evaluation of electrospun nanofibers containing pectin and ti...Nanomedicine Journal (NMJ)
Objective(s):The aim of this study was to prepare electrospun nanofibers of celecoxib using combination of time-dependent polymers with pectin to achieve a colon-specific drug delivery system for celecoxib.
Materials and Methods:Formulations were produced based on two multilevel 22 full factorial designs. The independent variables were the ratio of drug:time-dependent polymer (X1) and the amount of pectin in formulations (X2). Electrospinning process was used for preparation of nanofibers. The spinning solutions were loaded in 5 mL syringes. The feeding rate was fixed by a syringe pump at 2.0 mL/h and a high voltage supply at range 10-18 kV was applied for electrospinning. Electrospun nanofibers were collected and evaluated by scanning electron microscopy and drug release in the acid and buffer with pH 6.8 with and without pectinase.
Results:Electrospun nanofibers of celecoxib with appropriate morphological properties were produced via electrospinning process. Drug release from electrospun nanofibers was very low in the acidic media; while, drug release in the simulated colonic media was the highest from formulations containing pectin.
Conclusion: Formulation F2 (containing drug:ERS with the ratio of 1:2 and 10% pectin) exhibited acceptable morphological characteristics and protection of drug in the upper GI tract and could be a good candidate as a colonic drug delivery system for celecoxib.
The combined effects of Aloe vera gel and silver nanoparticles on wound heali...Nanomedicine Journal (NMJ)
Objective(s): This study was aimed at investigating the synergy effects of Aloe vera gel and silver nanoparticles on the healing rate of the cutting wounds.
Materials and Methods: In order to determine the concentration of silver nanoparticles in Aloe vera gel, the MBC methods were applied on the most common bacteria infecting wounds, Staphylococcus aureus, Escherichia coli, Pseudomonas aeruginosa. The cutting wounds with Full-thickness skin were dorsally created on rats; then the rats were divided into 4 groups. The treatments groups included: mixture of Aloe vera gel and silver nanoparticles, Aloe vera gel alone and silver nanoparticles alone in addition to control groups. The treatment was carried out for 2 weeks and the size of the wound closures were measured by an image software analysis.
Results:There was no significant difference (p<0.05) in healing rate between the control and mixture group. However, there were significant differences between the silver nanoparticles and Aloe vera groups using Tukey’s analysis on the 6th, 8th and 10th days.
Conclusion:The Aloe vera gel increased the rate of wound healing whereas the silver nanoparticles had a delay effect; and when they were mixed, it was similar to the average effect of both Aloe vera gel and silver nanoparticles.
Antimicrobial and cytotoxicity effect of silver nanoparticle synthesized by C...Nanomedicine Journal (NMJ)
Objective(s): For the development of reliable, ecofriendly, less expensive process for the synthesis of silver nanoparticles and to evaluate the bactericidal, and cytotoxicity properties of silver nanoparticles synthesized from root extract of Croton bonplandianum, Baill.
Materials and Methods: The synthesis of silver nanoparticles by plant part of Croton bonplandianum was carried out. The formation of nanoparticles was confirmed by Transmission Electron Microscopy (TEM), Scanning Electron Microscopy (SEM), XRD and UV-Vis spectrophotometric analysis. The biochemical properties were assayed by antibacterial study, cytotoxicity assay using cancer cell line.
Results: The formation of silver nanoparticles was confirmed by UV-VIS spectroscopic analysis which showed absorbance peak at 425 nm. X-ray diffraction photograph indicated the face centered cubic structure of the synthesized AgNPs. TEM has displayed the different dimensional images of biogenic silver nanoparticles with particle size distribution ranging from 15-40 nm with an average size of 32 nm. Silver particles are spherical in shape, clustered. The EDX analysis was used to identify the elemental composition of synthesized AgNPs. Antibacterial activity of the synthesized AgNPs against three Gram positive and Gram negative bacteria strains like Staphylococcus aureus, Escherichia coli and Pseudomonas aeruginosa carried out showed significant zones of inhibition. The cytotoxicity study by AgNPS also showed cytotoxicity on ovarian cancer cell line PA-1 and lung epithelial cancer cell line A549.
Conclusion: The present study confirms that the AgNPs have great promise as antibacterial, and anticancer agent.
Investigation of the effect of different parameters on the phase inversion te...Nanomedicine Journal (NMJ)
Objective(s): Nanoemulsions are a kind of emulsions that can be transparent, translucent (size range 50-200 nm) or “milky” (up to 500 nm). Nanoemulsions are adequatly effective for transfer of active component through skin which facilitate the entrance of the active component . The transparent nature of the system and lack of the thickener and fluidity are among advantages of nanoemulsion.
Materials and Methods: In this study, a nanoemulsion of lemon oil in water was prepared by the phase inversion temperature (PIT) emulsification method in which the tween 40 was used as surfactant. The effect of concentration of NaCl in aqueous phase, pH and weight percent of surfactant and aqueous on the PIT and droplet size were investigated. Results: The results showed that with increasing of concentration of NaCl from 0.05 M to 1 M, PIT decrease from 72 to 50. The average droplet sizes, for 0.1, 0.5 and 1 M of NaCl in 25 ºC are 497.3, 308.1 and 189.9 nm, respectively and the polydispersity indexes are 0.348, 0.334 and 0.307, respectively.
Conclusion: Considering the characteristics of nanoemulsions such as being transparent, endurance of solution and droplet size can provide suitable reaction environment for polymerization process used in making hygienic and medical materials.
Mechanism of oxidative stress involved in the toxicity of ZnO nanoparticles a...Nanomedicine Journal (NMJ)
ZnO NPs (zinc oxide nanoparticles) has generated significant scientific interest as a novel antibacterial and anticancer agent. Since oxidative stress is a critical determinant of ZnO NPs-induced damage, it is necessary to characterize their underlying mode of action. Different structural and physicochemical properties of ZnO NPs such as particle surface, size, shape, crystal structure, chemical position, and presence of metals can lead to changes in biological activities including ROS (reactive oxygen species) production. However, there are some inconsistencies in the literature on the relation between the physicochemical features of ZnO NPs and their plausible oxidative stress mechanism. Herein, the possible oxidative stress mechanism of ZnO NPs was reviewed. This is worthy of further detailed evaluations in order to improve our understanding of vital NPs characteristics governing their toxicity. Therefore, this study focuses on the different reported oxidative stress paradigms induced by ZnO NPs including ROS generated by NPs, oxidative stress due to the NPs-cell interaction, and role of the particle dissolution in the oxidative damage. Also, this study tries to characterize and understand the multiple pathways involved in oxidative stress induced by ZnO NPs. Knowledge about different cellular signaling cascades stimulated by ZnO NPs lead to the better interpretation of the toxic influences induced by the cellular and acellular parameters. Regarding the potential benefits of toxic effects of ZnO NPs, in-depth evaluation of their toxicity mechanism and various effects of these nanoparticles would facilitate their implementation for biomedical applications.
Combined effects of PEGylation and particle size on uptake of PLGA particles ...Nanomedicine Journal (NMJ)
Abstract
Objective:
At the present study, relationship between phagocytosis of PLGA particles and combined effects of particle size and surface PEGylation was investigated.
Materials and Methods:
Microspheres and nanospheres (3500 nm and 700 nm) were prepared from three types of PLGA polymers (non-PEGylated and PEGylation percents of 9% and 15%). These particles were prepared by solvent evaporation method. All particles were labeled with FITC-Albumin. Interaction of particles with J744.A.1 mouse macrophage cells, was evaluated in the absence or presence of 7% of the serum by flowcytometry method.
Results:
The study revealed more phagocytosis of nanospheres. In the presence of the serum, PEGylated particles were phagocytosed less than non-PEGylated particles. For nanospheres, this difference was significant (P<0/05) and their uptake was affected by PEGylation degree. In the case of microsphere formulation, PEGylation did not affect the cell uptake. In the serum-free medium, the bigger particles had more cell uptake rate than smaller ones but the cell uptake rate was not influenced by PEGylation.
Conclusion:
The results indicated that in nanosized particles both size and PEgylation degree could affect the phagocytosis, but in micron sized particles just size, and not the PEGylation degree, could affect this.
Synthesis of silver nanoparticles and its synergistic effects in combination ...Nanomedicine Journal (NMJ)
Abstract
Objectives:
Biofilms are communities of bacteria attached to surfaces through an external polymeric substances matrix. In the meantime, Acinetobacterbaumannii is the predominant species related to nosocomial infections. In the present study, the effect of silver nanoparticles alone and in combination with biocides and imipenem against planktonic and biofilms of A. baumannii was assessed.
Materials and Methods:
Minimum inhibitory concentrations (MICs) of 75 planktonic isolates of A. baumannii were determined by using the microdilution method as described via clinical and laboratory standards institute (CLSI). Among all strains, 10 isolates which formed strong biofilms were selected and exposed to silver nanoparticles alone and in combination with imipenem, bismuth ethandithiol (BisEDT) and bismuth propanedithiol (BisPDT) to determine minimum biofilm inhibitory concentrations (MBIC). Subsequently, minimum biofilm eradication concentrations (MBECs) of silver nanoparticles alone and in combination with imipenem against mature biofilm of the isolates were evaluated.
Results:
Results showed that 29.3% of isolates were susceptible to silver nanoparticles and could inhibit the growth and eradicate biofilms produced by the isolates. For this reason, ∑FIC, ∑FBIC and ∑FBEC ≤ 0.05 were reported which shows synergism between silver nanoparticles and imipenem against not only planktonic cells but also inhibition and eradication of biofilms. The results of ∑FBIC >2 indicated to antagonistic impacts between silver nanoparticles and BisEDT/BisPDT against biofilms.
Conclusion:
It can be concluded that silver nanoparticles alone can inhibit biofilm formation but in combination with imipenem are more effective against A. baumannii in planktonic and biofilm forms.
Abstract
Objective(s):
Zinc oxide nanoparticles (ZNP) are increasingly used in sunscreens, biosensors, food additives and pigments. In this study the effects of ZNP on liver of rats was investigated.
Materials and Methods:
Experimental groups received 5, 50 and 300 mg/kg ZNP respectively for 14 days. Control group received only distilled water. ALT, AST and ALP were considered as biomarkers to indicate hepatotoxicity. Lipid peroxidation (MDA), SOD and GPx were detected for assessment of oxidative stress in liver tissue. Histological studies and TUNEL assay were also done.
Results:
Plasma concentration of zinc (Zn) was significantly increased in 5 mg/kg ZNP-treated rats. Liver concentration of Zn was significantly increased in the 300 mg/kg ZNP-treated animals. Weight of liver was markedly increased in both 5 and 300 mg/kg doses of ZNP. ZNP at the doses of 5 mg/kg induced a significant increase in oxidative stress through the increase in MDA content and a significant decrease in SOD and GPx enzymes activity in the liver tissue. Administration of ZNP at 5 mg/kg induced a significant elevation in plasma AST, ALT and ALP. Histological studies showed that treatment with 5 mg/kg of ZNP caused hepatocytes swelling, which was accompanied by congestion of RBC and accumulation of inflammatory cells. Apoptotic index was also significantly increased in this group. ZNP at the dose of 300 mg/kg had poor hepatotoxicity effect.
Conclusion:
It is concluded that lower doses of ZNP has more hepatotoxic effects on rats, and recommended to use it with caution if there is a hepatological problem.
Synthesis of graphene oxide-TiO2 nanocomposite as an adsorbent for the enrich...Nanomedicine Journal (NMJ)
Abstract
Objective(s):
In our study, graphene oxide-TiO2 nanocomposite (GO/TiO2) was prepared and used for the enrichment of rutin from real samples for the first time.
Materials and Methods:
The synthesized GO/TiO2 was characterized by X-ray diffraction, scanning electron microscopy, and FT-IR spectra. The enrichment process is fast and highly efficient. The factors including contact time, pH, and amount of GO/TiO2 affecting the adsorption process were studied.
Results:
The maximum adsorption capacity for ciprofloxacin was calculated to be 59.5 mg/g according to the Langmuir adsorption isotherm. The method yielded a linear calibration curve in the concentration ranges from 15 to 200 μg/L for the rutin with regression coefficients (r2) of 0.9990. The limits of detection (LODs, S/N=3) and limits of quantification (LOQs, S/N=10) were found to be 8 μg/Land 28 μg/L, respectively. Both the intra-day and inter-day precisions (RSDs) were < 10% .
Conclusion:
The developed approach offered wide linear range, and good reproducibility. Owing to the diverse structures and unique characteristic, GO/TiO2 possesses great potential in the enrichment and analysis of trace rutin in real aqueous samples.
Preparation and evaluation of vitamin A nanosuspension as a novel ocular drug...Nanomedicine Journal (NMJ)
Abstract
Objective(s):
The aim of this study was to prepare a nanosuspension formulation as a new vehicle for the improvement of the ocular delivery of vitamin A.
Material and Methods:
Formulations were designed based on full factorial design. A high pressure homogenization technique was used to produce nanosuspensions. Fifteen formulations were prepared by the use of different combinations of surfactants Tween 80, benzalkonium chloride and Pluronic and evaluated for pH, particle size, entrapment efficiency, differential scanning calorimetry (DSC), stability and drug release. Also, Draize test was used to evaluate the irritation of rabbit eye by formulations.
Results:
All formulations showed a small mean size that is well suited for ocular application. Also it was observed that the particle size decreased with increase in the amount of surfactant. Drug entrapment increased with increasing amount of surfactant. It was shown that initial and final drug release can be controlled by the ratio and the total amount of surfactants, respectively.
Conclusion:
It was concluded that the use of Tween 80 and Pluronic in the formualtions with a proper ratio does not show eye irritation and could be useful to achieve a suitable nanosuspension of vitamin A as a novel ocular delivery system.
A comparative study about toxicity of CdSe quantum dots on reproductive syste...Nanomedicine Journal (NMJ)
This study examined the toxicity of CdSe quantum dots (QDs) and CdSe:ZnS QDs on the reproductive system of mice. Mice were injected with doses of 10, 20, and 40 mg/kg of CdSe QDs or CdSe:ZnS QDs. Histological analysis found that the 40 mg/kg dose of CdSe:ZnS QDs caused abnormal growth of seminiferous tubes, impaired spermatogenesis, and a decrease in testis weight, sperm count, and testosterone levels compared to controls. The CdSe:ZnS QDs at 40 mg/kg also decreased sperm density in the epididymis. This suggests that, contrary to previous reports, the
Functionalization of carbon nanotubes and its application in nanomedicine: A ...Nanomedicine Journal (NMJ)
Abstract
This review focuses on the latest developments in applications of carbon nanotubes (CNTs) in medicine. A brief history of CNTs and a general introduction to the field are presented.
Then, surface modification of CNTs that makes them ideal for use in medical applications is highlighted. Examples of common applications, including cell penetration, drug delivery, gene delivery and imaging, are given. At the same time, there are concerns about their possible adverse effects on human health, since there is evidence that exposure to CNTs induces toxic effects in experimental models. However, CNTs are not a single substance but a growing family of different materials possibly eliciting different biological responses. As a consequence, the hazards associated with the exposure of humans to the different forms of CNTs may be different. Understanding the structure–toxicity relationships would help towards the assessment of the risk related to these materials. Finally, toxicity of CNTs, are discussed. This review article overviews the most recent applications of CNTs in Nanomedicine, covering the period from 1991 to early 2015.
The role of surface charge of ISCOMATRIX nanoparticles on the type of immune ...Nanomedicine Journal (NMJ)
Abstract
Objective(s):
ISCOMATRIX vaccines have now been shown to induce strong antigen-specific cellular or humoral immune responses to a broad range of antigens of viral, bacterial, parasite or tumor. In the present study, we investigated the role of ISCOMATRIX charge in induction of a Th1 type of immune response and protection against Leishmania major infection in BALB/c mice.
Materials and Methods:
Positively and negatively charged ISCOMATRIX were prepared. BALB/C mice were immunized subcutaneously, three times with 2-week intervals, with different ISCOMATRIX formulations. Soluble Leishmania antigens (SLA) were mixed with ISCOMATRIX right before injection. The extent of protection and type of immune response were studied in different groups of mice.
Results:
The group of mice immunized with negatively charged ISCOMATRIX showed smaller footpad swelling upon challenge with L. major and the highest IgG2a production compared with positively charged one. The mice immunized with positively charged ISCOMATRIX showed the lowest splenic parasite burden compared to the other groups. Cytokine assay results indicated that the highest level of IFN- γ and IL-4 secretion was observed in the splenocytes of mice immunized with negatively charged ISCOMATRIX as compared to other groups.
Conclusion:
The results indicated that ISCOMATRIX formulations generate an immune response with mixed Th1/Th2 response that was not protective against challenge against L. major.
This document discusses the use of nanotechnology in cancer treatment and photodynamic therapy (PDT). It first introduces quantum dots (QDs), which are spherical semiconductor nanoparticles that have attractive optical properties for biomedical applications. QDs can be functionalized for targeted cancer therapy and have also been explored as photosensitizers for PDT. The document then provides background on PDT, describing its mechanisms of action and how it uses photosensitizers activated by light to generate reactive oxygen species that damage tumor cells. The potential advantages of PDT over conventional cancer therapies are noted. Finally, the document discusses how QDs, due to their tunable light absorption, have potential as novel photosensitizers for PDT to improve
This document discusses the use of nanotechnology in cancer treatment and photodynamic therapy. It focuses on the use of quantum dots, which are spherical nanoparticles that have attractive optical properties like high photoluminescence, narrow emission spectra, and photostability. These properties make quantum dots useful as photosensitizers for photodynamic therapy of cancer tumors. The document reviews how quantum dots can be functionalized and targeted to cancer cells for photodynamic therapy applications. It also evaluates the design of nanoparticles and their potential safety for biomedical uses.
Preparation of protein-loaded PLGA-PVP blend nanoparticles by nanoprecipitati...Nanomedicine Journal (NMJ)
Abstract
Objective(s):
Despite of wide range applications of polymeric nanoparticles in protein delivery, there are some problems for the field of protein entrapment, initial burst and controlled release profile.
Materials and Methods:
In this study, we investigated the influence of some changes in PLGA nanoparticles formulation to improve the initial and controlled release profile. Selected parameters were: pluronic F127, polysorbate 80 as surfactant, pH of inner aqueous phase, L/G ratio of PLGA polymer, volume of inner aqueous phase and addition of polyvinylpyrrolidone as an excipient. FITC-HSA was used as a model hydrophilic drug. The nanoparticles were prepared by nanoprecipitation.
Results:
Initial release of FITC-HSA from PLGA-tween 80 nanoparticles (opt-4, 61%) was faster than control (PLGA-pluronic) after 2.30 h of incubation. Results showed that decrease in pH of inner aqueous phase to pI of protein can decrease IBR but the release profile of protein is the same as control. Release profile with three phases including a) initial burst b) plateau and c) final release phase was observed when we changed volume of inner aqueous phase and L/G ratio in formulation. Co-entrapment of HSA with PVP and pluronic reduced the IBR and controlled release profile in opt-19. Encapsulation efficiency was more than 97% and nanoparticles size and zeta potentials were mono-modal and -18.99 mV, respectively.
Conclusion:
In this research, we optimized a process for preparation of PLGA-PVP-pluronic nanoparticles of diameter less than 300 nm using nanoprecipitation method. This formulation showed a decreased initial burst and long lasting controlled release profile for FITC-HSA as a model drug for proteins.
Abstract
Objective(s):
Abdominal adhesions are one of the most important problems, occurring after intra-abdominal surgery in more than 90% of cases. This condition is the leading cause of bowel obstruction, infertility, and abdominal/pelvic pain. Gold nanoparticles (GNPs) have been shown to be non-toxic and exhibit anti-inflammatory, anti-angiogenic and antioxidant activities. The purpose of this study was to determine the effect of intraperitoneal lavage with GNP solutions on the development of postoperative peritoneal adhesion (PPA).
Materials and Methods:
In the current experimental study, thirty-five male Wistar rats were randomly assigned to seven groups of five rats. After a standardized peritoneal injury, GNP solutions in different concentrations (1, 2.5, 5, 10, 50 and 100 ng/ml) were locally administered through nebulization; normal saline (NS) was administered to the control group. Two weeks later, the rats were sacrificed and cecum and peritoneal samples were harvested for histopathological assessment. Blood samples were obtained to determine serum concentrations of inflammatory biomarkers including tumor necrosis factor alpha (TNF-α), interleukin-1 beta (IL-1β) and vascular endothelial growth factor (VEGF).
Results:
The rats treated with GNPs had significantly lower microscopic and macroscopic peritoneal adhesion scores, compared to the control group (P<0.05). Score 5 of macroscopic adhesions was reported in all the rats of the control group, unlike the GNP groups. Furthermore, microscopic adhesions were reported with all rats in the control group, unlike the GNP groups (reported in 0 out of 5 rats in all GNP groups). In addition, serum levels of IL-1β, TNF-α and VEGF underwent no significant changes.
Conclusion:
Compared to the control group, GNPs decreased the severity of peritoneal adhesions, although they did not alter TNF-α, IL-1β or VEGF serum levels.
Applications of artificial Intelligence in Mechanical Engineering.pdfAtif Razi
Historically, mechanical engineering has relied heavily on human expertise and empirical methods to solve complex problems. With the introduction of computer-aided design (CAD) and finite element analysis (FEA), the field took its first steps towards digitization. These tools allowed engineers to simulate and analyze mechanical systems with greater accuracy and efficiency. However, the sheer volume of data generated by modern engineering systems and the increasing complexity of these systems have necessitated more advanced analytical tools, paving the way for AI.
AI offers the capability to process vast amounts of data, identify patterns, and make predictions with a level of speed and accuracy unattainable by traditional methods. This has profound implications for mechanical engineering, enabling more efficient design processes, predictive maintenance strategies, and optimized manufacturing operations. AI-driven tools can learn from historical data, adapt to new information, and continuously improve their performance, making them invaluable in tackling the multifaceted challenges of modern mechanical engineering.
We have designed & manufacture the Lubi Valves LBF series type of Butterfly Valves for General Utility Water applications as well as for HVAC applications.
Properties of Fluids, Fluid Statics, Pressure MeasurementIndrajeet sahu
Properties of Fluids: Density, viscosity, surface tension, compressibility, and specific gravity define fluid behavior.
Fluid Statics: Studies pressure, hydrostatic pressure, buoyancy, and fluid forces on surfaces.
Pressure at a Point: In a static fluid, the pressure at any point is the same in all directions. This is known as Pascal's principle. The pressure increases with depth due to the weight of the fluid above.
Hydrostatic Pressure: The pressure exerted by a fluid at rest due to the force of gravity. It can be calculated using the formula P=ρghP=ρgh, where PP is the pressure, ρρ is the fluid density, gg is the acceleration due to gravity, and hh is the height of the fluid column above the point in question.
Buoyancy: The upward force exerted by a fluid on a submerged or partially submerged object. This force is equal to the weight of the fluid displaced by the object, as described by Archimedes' principle. Buoyancy explains why objects float or sink in fluids.
Fluid Pressure on Surfaces: The analysis of pressure forces on surfaces submerged in fluids. This includes calculating the total force and the center of pressure, which is the point where the resultant pressure force acts.
Pressure Measurement: Manometers, barometers, pressure gauges, and differential pressure transducers measure fluid pressure.
3rd International Conference on Artificial Intelligence Advances (AIAD 2024)GiselleginaGloria
3rd International Conference on Artificial Intelligence Advances (AIAD 2024) will act as a major forum for the presentation of innovative ideas, approaches, developments, and research projects in the area advanced Artificial Intelligence. It will also serve to facilitate the exchange of information between researchers and industry professionals to discuss the latest issues and advancement in the research area. Core areas of AI and advanced multi-disciplinary and its applications will be covered during the conferences.
Open Channel Flow: fluid flow with a free surfaceIndrajeet sahu
Open Channel Flow: This topic focuses on fluid flow with a free surface, such as in rivers, canals, and drainage ditches. Key concepts include the classification of flow types (steady vs. unsteady, uniform vs. non-uniform), hydraulic radius, flow resistance, Manning's equation, critical flow conditions, and energy and momentum principles. It also covers flow measurement techniques, gradually varied flow analysis, and the design of open channels. Understanding these principles is vital for effective water resource management and engineering applications.
Impartiality as per ISO /IEC 17025:2017 StandardMuhammadJazib15
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Prediction of Electrical Energy Efficiency Using Information on Consumer's Ac...PriyankaKilaniya
Energy efficiency has been important since the latter part of the last century. The main object of this survey is to determine the energy efficiency knowledge among consumers. Two separate districts in Bangladesh are selected to conduct the survey on households and showrooms about the energy and seller also. The survey uses the data to find some regression equations from which it is easy to predict energy efficiency knowledge. The data is analyzed and calculated based on five important criteria. The initial target was to find some factors that help predict a person's energy efficiency knowledge. From the survey, it is found that the energy efficiency awareness among the people of our country is very low. Relationships between household energy use behaviors are estimated using a unique dataset of about 40 households and 20 showrooms in Bangladesh's Chapainawabganj and Bagerhat districts. Knowledge of energy consumption and energy efficiency technology options is found to be associated with household use of energy conservation practices. Household characteristics also influence household energy use behavior. Younger household cohorts are more likely to adopt energy-efficient technologies and energy conservation practices and place primary importance on energy saving for environmental reasons. Education also influences attitudes toward energy conservation in Bangladesh. Low-education households indicate they primarily save electricity for the environment while high-education households indicate they are motivated by environmental concerns.
Simultaneous diagnosis and drug delivery by silymarin-loaded magnetic nanoparticles
1. Nanomed. J., 2(3):223-230, Summer 2015
223
Simultaneous diagnosis and drug delivery by silymarin-loaded magnetic
nanoparticles
1
M. Khalkhali; 2
S. Sadighian; 3,4*
K. Rostamizadeh; 1
F. Khoeini;5
M. Naghibi; 2
N. Bayat; 3
M. Hamidi
1
Department of Physics, University of Zanjan, Zanjan, Iran
2
Department of Pharmaceutical biomaterials, School of Pharmacy, Zanjan University of Medical Sciences, Zanjan
Iran
3
Zanjan Pharmaceutical Nanotechnology Research Center, Zanjan University of Medical Sciences, Zanjan, Iran
4
Department of Medicinal Chemistry, School of Pharmacy, Zanjan University of Medical Sciences, Zanjan, Iran
5
Shahid Beheshti University of Medical Sciences, Tehran, Iran
ABSTRACT:
Objective(s): The aim of this work was to prepare and characterize magnetic nanoparticles (MNPs) as theranostic
system to act simultaneously as drug carrier and MRI contrast agent. Chitosan-coated MNPs (CMNPs) were prepared
and loaded with silymarin. Silymarin-loaded CMNPs were characterized with various techniques and their potential as
MRI contrast agent was also evaluated.
Materials and Methods: The chitosan-coated MNPs were prepared by coprecipitation method and were loaded with
silymarin. The synthesized nanoparticles were characterized by various techniques including SEM, TEM, X ray
diffraction (XRD), FTIR and vibrating sample magnetometer (VSM). In vitro drug release of silymarin was evaluated
at 37 ÚC at pH 5.3 and 7.4. Then, their proton relaxivity was evaluated to study the potential of CMNPs as MRI
contrast agent in terms of r1
and r2
.
Results: Silymarin-loaded CMNPs were successfully prepared and characterized by FTIR and XRD techniques. VSM
analysis revealed superparamagnetic properties of CMNPs. The release study showed that the maximum drug release
accessible for CMNPs in pH=5.3 was higher than pH=7.4. Finally, the r2
/r1
value of CMNPs was found to be close to
20 indicating that CMNPs has a strong efficiency as T2
contrast agents for MRI imaging.
Conclusion: The findings demonstrated the potential of CMNPs as efficient MRI contrast agent as well as silymarin
drug delivery.
Keywords: Chitosan, Drug delivery systems, Magnetite, MRI contrast agent, Silymarin
Nanomed. J., 2(3): 223-230, Summer 2015
ISSN 2322 - 5904
*Corresponding Author Email: rostamizadeh@zums.ac.ir
Tel.: (+98) 24134473635;
Note. This manuscript was submitted on March 26, 2015;
approved on June 15, 2015;
Received; 26 March 2015 Accepted; 15 June 2015
INTRODUCTION
Magnetic nanoparticles (MNPs) because of their
unique properties such as small size, super-
paramagnetism, low toxicity, etc, has found many
applications in biomedicine for disease diagnosis and
cancer therapy(e.g. MRI, drug deliverysystems (DDS),
hyperthermia) (1, 2). To get benefit of MNPs in
biomedicine, they should be stable for long term in
aqueous solution, have particle size of less than 100
nm, and possess high magnetization. In addition,
MNPs have to be coated in order to prevent the
agglomeration and provide uniform distribution in
suspension. There are different methods for preparation
of stable dispersion of iron oxide in organic solvents
including hexane and decane (3, 4). Infact, for biological
applications, it is vital to have stable MNPs in aqueous
solution. So, to increase the stability of MNPs in
aqueous solution, it is of great importance to use
stabilizers such as surfactants, oxide or polymer
compounds (especially bio-compatible polymer) with
some specific functional groups on the surface of
MNPs. In addition, the shell on the magnetic core
provides a lot of significant advantages. It helps to
2. Nanomed. J., 2(3):223-230, Summer 2015
224
M. Khalkhali et al.
improve physical and chemical properties of the MNPs.
It also has important role in protecting and stabilizing
the core against the influence of acid, alkaline and
oxidizing conditions, preparation of the nanoparticle
with a desired surface charge and chemical functional
group. Among different coatings, chitosan as a
naturally drived polymer has been used extensively
for modification of the surface MNPs owing to its
biocompatibility and biodegra- dability (5). Targeted
therapy and controlled drug delivery are the principal
aims of novel drug delivery systems. Carrier is the most
important component of DDS, and it should be non
toxic, should bind the drug properly, and make it
possible to release intended drug at the target site.
Currently, there are different kind of nanodrug delivery
systems consisting of polymeric nano- particle,
liposome, dan drimer and micelles (6). Indeed, the role
of nanoparticles (NP) is to improve their solubility,
improve the therapeutic value of applied drugs by
addition of retention time, and pass the biological
barriers (7, 8, 9). Nowadays, MNPs have attracted an
immense deal of attention for drug delivery systems
and MRI imaging (10,11). Milk thistle (Silybum
marianum, Asteraceae) seeds have been applied for
centuries as treatment for several illnesses especially
for liver. Silibinin, silychristin, and silidianin are the
main component of milk thistle seed collectively known
as silymarin extracted from milk thistle seeds, available
commercially as standardized extract. Silymarin and its
components (especially silibinin) have antioxidant, anti-
inflammatory, immunomodulatory, lipid and biliary
effects (12, 13). Silibinin shows membrane protective
confidants and it may protect blood constituents from
oxidative damage (14, 15). Silymarin shows low
absorbtion and bioavability (between 20 and 50%),
probably due to its degeneration by gastric fluid, poor
enteral absorption or poor water solubility (16,17, 18).
Several methods including using a buccal liposomal
delivery system (19), forming complexes with
phospholipids (18) and incorporation into solid
dispersions (20) have been reported to change the
bioavailability of silymarin or silybin. Short half-life,
low bioavailability and hydrophobic nature make it an
appropriate candidate for gastrore-tentive drug
delivery system. The MNPs can be used as drug carrier
for drugs with lipophilic nature owing the advantage
of being directed into the target tissue by its magnetic
section. PLGA-PEG-MNPs is a kind of DDS have been
reported where the pharmaceutical drugs was
conjugated to the surface of PLGA-PEG-MNPs
physically and released payload drug into the target
site due to its external localized magnetic-field gradient
(21, 22). In the present contribution, chitosan-coated
MNPs (CMNPs) were prepared and characterized as
theranostic system to act simultaneously as drug
carrier and MRI contrast agent. CMNPs were prepared
and loaded with silymarin. Silymarin-loaded CMNPs
were characterized with various techniques and their
potential as MRI contrast agent was evaluated.
MATERIALS AND METHODS
Experimental
Silymarin was a gift from Barij Essence
Pharmaceutical Company (Iran). Ferric chloride hexa-
hydrate (FeCl3
·6H2
O), ferrous chloride tetra-hydrate
(FeCl2
·4H2
O), NH4
OH (25% of ammonia), acetic acid
(75%) and all solvents were from Merck and purchased
locally. Chitosan was provided from Sigma. All the
materials were used without any purification.
Preparation of iron oxide nanoparticles (MNPs)
Briefly, 1.62 g of ferric chloride was dissolved in 60
ml distilled water (0.1 M) under nitrogen gas
atomosphere (23). Then, 0.6 g of ferrous chloride
dissolved in 30 ml of distilled water (0.1M), was added
and the solution mixed under nitrogen for 15 min. Then
diluted solution of NH3
was added dropwise to the
solution of iron salts when the color of the solution
immediately changed to dark black. The precipitate was
separated with strong external magnet (1.2 T) and
washed several times with distilled water to remove
any ions.
Preparation of chitosan-coated MNPs (CMNPs)
First, 20 mg of high molecular weight chitosan
dissolved in 1 M acetic acid solution with final volume
of 100 ml. Then 70 mg of MNPs were added to the
solution and the mixture was mixed for 18 h.During this
process, chitosan molecules were adsorbed on the
surface of the MNPs and a dark brown suspension
was obtained.
Preparation of silymarin-loaded CMNPs
Briefly, 50 mg CMNPs was added into 10 mg of
silymarin (preliminarily solubilized in 5 ml ethanol) and
stirred for 20 h. The silymarin-loaded CMNPs were
separated by centrifugation at 14000 rpm and then
washed three times with deionized water.The silymarin-
3. Nanomed. J., 2(3):223-230, Summer 2015
225
entrapped nanoparticles were dried in vacuumed oven at
30 ºC for12 h.Theunloaded silymarinwasdetermined by
measuring the concentration of drug in supernatant of
centrifugation by UV-Vis spectrophotometry at
wavelength of 288 nm. The entrapment efficiency was
calculated using the following equation:
EntapmentEfficiency(%)=(Total amountofdrug-free
amount of drug) / Total amount of drug (1)
Drug release study
The drug release behavior of nanoparticles were
studied in physiological pH of 7.4 and acidic media with
the pH of 5.3 in phosphate-buffered saline, PBS
containing 0.5% (w/v) Tween 80. Typically, 10 mg of
nanoparticles were placed into a dialysis bag (cut off 12
kDa) and introduced to 15 mL of PBS with desired pH
under stirring (100 rpm) at 37 °C.At predetermined time
intervals, in order to determine the drug concentration in
dialysateand therebytime-dependentdrugreleaseprofile,
1.0 mL of dialysate was taken out and replaced with 1.0
mLoffreshbuffersolutionmaintainedat37°Candassayed
by UV–Vis spectroscopy at wavelength of 288 nm.
Characterization techniques
FT-IRspectraofnanoparticlesweretakenwithaBruker
FT–IR spectrophotometerin the range of400–4000 cm–1
as KBr disks. The morphology of the chitosan-coated
MNPs was studied by field-emission scanning electron
microscopy (FESEM, Mira 3-XMU). The magnetic
properties of MNPs and the chitosan-coated MNPs were
measured in vibrating sample magnetometer (VSM,
LakeShore 7400) with an applied field between -20 to 20
kOeat25ÚC.Theparticlesizedistributionoftheprepared
CMNPswasdeterminedbydynamiclightscattering(DLS)
(MalvernInstruments,UK,modelNano ZS).Thestructure
and crystal phase of the CMNPs were measured by a
BrukerD8X-raydiffractometerwithmonochromatedhigh-
intensityCuKaradiation(k=1.5418 Å)operated at40 kV
and 30 mA.
Magnetic resonance imaging (MRI) measurements
For measuring the magnetic relaxation property ofthe
synthesized materials, MR imaging of CMNPs solutions
with differentironconcentrations of0, 25,50,75,100 and
200 µM were performed by using a clinical 1.5 T whole
body magnetic resonance (MR) scanner (Siemens
Healthcare Avanto Germany) at 25æ%
C. T1
images were
measured with applying the spin echo imaging sequence
at various repetition times of 100, 1550, 3150, 4750 and
6400 ms with an echo time of 18 ms, slice thickness: 7.5
mm,fieldofview(FOV):230,andmatrix:200×256.TheT2
images were obtained by using in the spin echo sequence
with repetition times (TR) of 1600 ms and varying echo
time(TE)of10,43,75,108and140ms,slicethickness:7.5
mm, field of view (FOV): 238, Turbo factor: 18, matrix:
176×384.Signal intensity with respect to each
concentrationwasextractedfromtheresultingMRIimages
and Dicom Works 1.3.5 software and used to determine
signal intensities within a manually drawn region of
interest (ROI) for each sample. The signal intensity vs.
TR or TE functions was exponentially fitted to the
followingequations(24,25).
]exp1[
1
0
T
TR
MI (2)
2
0 exp
T
TE
MI (3)
where I is the signal intensity and M0
is constants.
The longitudinal relaxivity r1
and transverse relaxivity r2
,
which represent the performance of the chitosan-coated
MNPs as contrast agents, are calculated from the slope
of the linear relationships.
RESULTS AND DISCUSSION
CMNPs with high dispersion capacity in aqueous
solution provide stable ferrofluids which can be used for
variousbiomedicalapplications(i.e.drugdeliverysystems
and diagnostics). Moreover, the nanocarrier composed
of magnetite nanoparticles can direct the payload drug
toward the tumor sites with the support of an external
magnetic field. On the other hand, because of the drug
encapsulation via electrostatic bonding, they possess
the capability to release the drug in the low-physiologic
pH environments(pH5–5.5),therebytargetingthe lower-
than-normal pH of the tumor sites as well as the media
present in the endosomes of the cancer cells. The FT-IR
spectraofCMNPs,silymarinandsilymarin-loadedCMNPs
are shown in Fig. 1.As shown in Fig 1a, the spectrum of
CMNPsexhibited the absorption peaksat1648,and 3274
cm-1
which can be attributed to N-H bending vibration
and stretching vibration of amine functional group of
chitosan, respectively. A strong absorption band at 557
cm-1
is characteristic peak of Fe-O band. Considering the
chemical structure of chitosan and MNPs, hydroxyl and
amino groups of chitosan form strong interaction with
the surfaces of MNPs (27). Fig 1b displays spectrum of
4. Nanomed. J., 2(3):223-230, Summer 2015
226
Silymarin-loaded magnetic nanoparticles as theranostic system
silymarin, peak at 1642 cm-1
is related to stretch vibration
of -C=C- alkenes and absorption band at 1462 cm-1
is
attributed tostretchingvibrationof C-Cbandsofaromatic
groups. Fig 1c displays silymarin-loaded CMNPs.
Apparently, the peakat 1642 cm-1
was shifted to 1591 cm-
1
, and thepeak at 557 cm-1
shifted to 569 cm-1
persumably
due to the association between silymarin and CMNPs.
Clearly, mainabsorption peaks ofsilymarinand chitosan-
coated MNPs were appeared in the spectrum silymarin-
loaded CMNPs indicating the successful silymarin
payload into CMNPs.Fig 2shows thecrystalline structure
of MNPs. Sevendiffraction peaks(2q (111),(220),(311),
(400),(422),(511)and(440))wereidentifiedinXRDpattern
demonstrating the inverse spinel structure of MNPs.
After coating chitosan on MNPs, no significant change
was observed. Using Debye Scherer’s formula, the
average nanoparticle size was calculated for uncoated
and chitosan-coated MNPs to be 10.48 and 8.25 nm,
respectively. The results show that the aggregation
degree of the CMNPs is smaller than that of the naked
MNPs.VSM graphs of MNPs and CMNPs are displayed
in Fig. 3. Clearly, both of MNPs and CMNPs show
superparamagnetic behaviors. As it is clear, the
saturation magnetization of CMNPs was slightly lesser
than that of MNPs. The reason behind this observation
can be explained by the presence of chitosan on the
surface of MNPs. Generally, it can be concluded that
CMNPs has adequate superparamagnetic properties
and could respond well to magnetic fields as a magnetic
drug carrier for targeted delivery and MRI imaging.
Size and zeta potential measurements
The size of nanoparticles was analyzed by DLS
technique. Particle size distribution curves showed only
one peak with a relatively low polydispersity index.
DLS histograms (Fig. 4 A and B) showed the particle
size of MNPs and CMNPs to be 126 nm and 32 nm,
respectively. The shape and morphology of
nanoparticles were shown in Fig. 4 C-E. According to
the Fig. 4C, the MNPs are in semi-spherical shape with
mean size of 55 nm. Fig. 4D displays CMNPs in the
same shape of the naked MNPs (4C),except the size of
CMNPs which decreased to 18 nm. Fig. 4E shows TEM
image of CMNPswith the average size of12 nm. Indeed,
different size obtained with DLS technique and SEM
image can be explained by the fact that in spite of SEM
image, DLS results imply to the hydrodynamic diameter
of nanoparticles, while SEM results correspond to the
particle size in dry condition. The zeta potentials of the
naked MNPs in aqueous dispersion were determined
to be -24.2 mV. Following coating MNPs with chitosan,
zeta potential increased to + 31.6 mV demonstrating
the presence of plentiful amino group of chitosan on
the surface of targeting carrier (Fig 4F and G).
Drug loading and “In vitro” drug release studies
The results revealed that the drug loading and
encapsulation efficiency for CMNPs were 10% and
95%, respectively. Fig 5 illustrates the drug release
response of the CMNPs in PBS (0.1% Tween 80) with
two different pH values of 5.3 and 7.4 at the
physiological temperature of 37 °C. Clearly, there was
no high initial burst release probably due to
hydrophobic nature of silymarin. As it can be seen,
silymarin-loaded CMNPs exhibited a sustained drug
release over six days at pH 5.3 with the maximum
attainable drug release close to 85 %. Controlled drug
release characteristic of CMNPs verify the capability
of these nanoparticles to be used as an impressive
carrier in silymarin delivery system.
MRI contrast enhancement
The longitudinal (T1
) and transverse (T2
) relaxation
times were measured at various solutions of different
iron concentrations using a clinical 1.5 T whole body
magnetic resonance (MR) scanner. Fig. 6 shows T1
-
weighted MR images of chitosan-coated MNPs with
iron concentrations of 0, 25, 50, 75, 100 and 200 µM in
deionized water. It illustrates a dose dependent signal
change which is due to the relaxation increase of the
water proton with increasing the dose. The magnetic
susceptibility of the iron oxide nanoparticles produce
local field gradients that accelerates the dephasing of
the spins of the surrounding water molecules and
raises spin–spin relaxation time (T2
). Fig. 7 shows T2
-
nanoparticles
r1
(mM-1
s-1
)
R2 r2
(mM-1
s-1
)
R2
r2/r1
chitosan
coated
MNPs
4.708 0.799 91.44 0.943 19.42
Table 1. The longitudinal relaxivity (r1
, mM”1
s”1
), transverse
relaxivity (r2
, mM”1
s”1
), r2
/r1
values and R2
of chitosan-coated
magnetite nanoparticles was calculated by plotting the
T1
relaxation rate (1/T1
) and T2
relaxationrate (1/T2
) as a
function of Fe concentration.
5. Nanomed. J., 2(3):223-230, Summer 2015
227
Fig. 1. FT-IR spectra of (a) CMNPs (b) silymarin (c) silymarin loaded CMNPs
Fig. 2. XRD pattern of (a) MNPs and (b) CMNPs
1 0 2 0 3 0 4 0 5 0 6 0 7 0
[422]
[440]
[511]
[400]
[311]
[220]
M N P s
C h ito s a n c o a te d M N P s
2 th e ta (d e g )
Intensity/a.u.
[111]
a
c
- 2 0 0 0 0 - 1 5 0 0 0 - 1 0 0 0 0 - 5 0 0 0 0 5 0 0 0 1 0 0 0 0 1 5 0 0 0 2 0 0 0 0
- 1 0 0
- 8 0
- 6 0
- 4 0
- 2 0
0
2 0
4 0
6 0
8 0
1 0 0
C h i t o s a n c o a t e d M N P s
a
b
H ( O e )
Magnetization(emu/g)
M N P s
Fig. 3. VSM curves of (a) MNPs and (b) CMNPs
6. Nanomed. J., 2(3):223-230, Summer 2015
228
M. Khalkhali et al.
A B
4 6 4 8 5 0 5 2 5 4 5 6 5 8 6 0 6 2 6 4 6 6
0 .0
0 .5
1 .0
1 .5
2 .0
2 .5
3 .0
3 .5
4 .0
Frequency
P a r ti c le S i z e ( n m )
C
E
F
G
Fig. 4. Size distribution of (A) MNPs (B) CMNPs assessed by DLS, (C) FESEM image of MNPs, (D) CMNPs, (E) TEM image of
CMNPs, and (F) zeta potential of MNPs (G) and CMNPs (F)
7. Nanomed. J., 2(3):223-230, Summer 2015
229
weighted MR images of CMNPs with different iron
concentration and illustrates a signal drop of the
phantom images with increasing iron concentration.
The r1
and r2
were calculated to be 4.708 and 91.44
mM”1
s”1
from the slopes of the 1/T1
(R1
) and 1/T2
(R2
)
plots versus Fe concentration, respectively (Fig. 7 and
Fig. 8). The calculated r1
, r2
and r2
/r1
values are shown in
Table 1. It has been reported that magnetic
nanoparticles are commonly used as T2
MRI contrast
agents and consequently they are able to decrease the
MR signal intensity (28). The efficiency of a contrast
agent is determined by ratio between transverse and
longitudinal relaxivity (r2
/r1
). The r2
/r1
ratio for CMNPs
was determined to be 19.42 which is higher than that of
Resovist, commercially available MRI contrast agent
(29). This finding indicates that CMNPs could be
considered as promising T2 contrast agent with strong
T2
shortening effect.
CONCLUSIONS
In the present study, a novel CMNPs was
synthesized by co-precipitation method. Chitosan was
selected to provide steric stabilization around MNPs and
provide stable aqueous dispersion. The FT-IR confirmed
the successful synthesis ofCMNPs. Particle size analysis
(DLS)andscanningelectronmicroscopy(SEM)confirmed
the formation of spherical nanoparticles with the final
average particle size about 18 nm. The VSM analysis
demonstrated thesaturationmagnetizationvaluesof29.08
Fig. 5. In vitro drug release profile of silymarin from CMNPs at
pH= 5.3 and 7.4
Fig . 6. T1
-weighted MRI images (1.5T, spin-echo sequence:
repitition time TR = 1550 ms, echo time TE = 18 ms) of
the CMNPs at various iron concentration at 25°C
Fig .7. T2
-weighted MRI images (1.5T, spin-echo sequence:
repitition time TR = 1600 ms, echo time TE = 108 ms) of the
CMNPs at various iron concentration at 25°C
Fig. 8. T1
relaxation rate plotted as a function of Fe
concentration (mM) for CMNPs
Fig. 9. T2
relaxation rate plotted as a function of Fe
concentration (mM) for CMNPs
8. Nanomed. J., 2(3):223-230, Summer 2015
230
M. Khalkhali et al.
emu/g for CMNPs. Entrapment efficiency and drug
loading for silymarin were calculated to be 95 and 10%,
respectively. The finding revealed that CMNPsprovide a
sustained release pattern. It was found that the maximum
drug releaseaccessible for CMNPs in pH=5.3 was higher
than pH=7.4. The the r2
/r1
value of CMNPs was
determined to be 19.42 indicating that the developed
formulation has a strong efficiency as T2
contrast agents
and controlled silymarin delivery.
ACKNOWLEDGMENT
We are most grateful for the continuing ûnancial
support of this research project by Zanjan University of
Medical Sciences and University of Zanjan.
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How to cite this article:
Khalkhali M, Sadighian S, Rostamizadeh K, Khoeini F, Naghibi M, bayat N, Hamidi M. Simultaneous diagnosis and drug delivery by silymarin-
loaded magnetic nanoparticles. Nanomed. J., 2015; 2(3): 223- 230.