This document discusses liposomes, which are spherical vesicles made of phospholipid bilayers that can encapsulate drugs. It provides details on the structure of liposomes, including their phospholipid and cholesterol components. Methods of preparing and characterizing liposomes are described. Applications include drug delivery for cancer, vaccines, and ophthalmic conditions. Marketed liposome drugs are highlighted.
The document discusses Good Laboratory Practices (GLP), which are regulations created by the FDA in 1978 that provide a framework for conducting laboratory studies. GLP was established in response to cases of poor laboratory practices including fraudulent activities and inaccurate reporting of results. The objectives of GLP are to ensure data submitted accurately reflects study results and is traceable. Laboratories must comply with requirements around facilities, equipment, recordkeeping, personnel qualifications and standard operating procedures to adhere to GLP. Noncompliance can result in disqualification and civil or criminal penalties for the laboratory.
The document discusses ocular drug delivery systems. It describes the anatomy and physiology of the eye and factors that influence drug absorption through the cornea. Various ocular drug delivery formulations are discussed including solutions, suspensions, emulsions, ointments, polymeric solutions, and particulate/vesicular systems. Recent advances include bioadhesive systems, collagen shields, pseudolatices, and penetration enhancers. Ocular inserts provide sustained drug release and increased bioavailability. Evaluation methods for these systems include in vitro drug release and in vivo studies in animals.
This document discusses the qualification phases for manufacturing equipment validation: design qualification, installation qualification, operational qualification, and performance qualification. It provides details on the objectives and contents of documentation for each phase. Design qualification establishes the basic design criteria. Installation qualification verifies proper installation. Operational qualification tests functionality under normal operating conditions without product. Performance qualification demonstrates the equipment operates as intended under actual use conditions with product. Re-qualification is also discussed.
This document discusses in process quality control (IPQC) for various dosage forms. IPQC involves monitoring products during manufacturing to ensure quality and prevent errors. It includes tests of raw materials, in-process materials, and finished products. The objectives are to monitor features affecting quality and prevent errors. IPQC is required by FDA cGMP guidelines. Specific IPQC procedures are described for parenteral products, solid dosage forms, and semisolid dosage forms. Records of IPQC must be reviewed and batches released by quality control.
Validation (intro, scope, merits, ich, who guidelines)PRAJAKTASAWANT33
This document summarizes a presentation on validation given by Prajakta Sawant, a first year M.Pharm student at Alard College of Pharmacy in Pune, India. The presentation covered the need for validation, types of validation including process, cleaning, equipment and analytical method validation. It discussed validation concepts such as the validation master plan, documentation, and ICH and WHO guidelines. The goal of validation is to ensure consistent production of pharmaceuticals meeting quality standards.
Buccal Drug Delivery System Mali vv pptVidhyaMali1
BDDS refers to drug delivery systems that administer drugs through the buccal mucosa in the oral cavity. The buccal mucosa has a rich blood supply and provides a non-invasive route for systemic drug delivery with advantages like rapid absorption and avoidance of first-pass metabolism. Formulations can be designed as solids, semisolids, or liquids depending on the drug properties and desired release characteristics. The drug permeates through the buccal mucosa via transcellular or paracellular routes to enter systemic circulation. Buccal delivery offers an alternative to oral and parenteral routes for certain drugs.
This document discusses buccal drug delivery and mucoadhesion. It begins by covering topics like the introduction, classification of drug delivery in the oral mucosa (buccal vs sublingual delivery), anatomy of the buccal mucosa, principle of mucoadhesion and theories of mucoadhesion. It then discusses buccal drug delivery in more detail - including its applications, advantages, limitations and various buccal dosage forms. The key highlights are buccal drug delivery avoids first pass metabolism, maintains drug levels longer than sublingual route, and uses mucoadhesive polymers and dosage forms like patches, tablets and gels for drug retention in the buccal cavity.
The document discusses Good Laboratory Practices (GLP), which are regulations created by the FDA in 1978 that provide a framework for conducting laboratory studies. GLP was established in response to cases of poor laboratory practices including fraudulent activities and inaccurate reporting of results. The objectives of GLP are to ensure data submitted accurately reflects study results and is traceable. Laboratories must comply with requirements around facilities, equipment, recordkeeping, personnel qualifications and standard operating procedures to adhere to GLP. Noncompliance can result in disqualification and civil or criminal penalties for the laboratory.
The document discusses ocular drug delivery systems. It describes the anatomy and physiology of the eye and factors that influence drug absorption through the cornea. Various ocular drug delivery formulations are discussed including solutions, suspensions, emulsions, ointments, polymeric solutions, and particulate/vesicular systems. Recent advances include bioadhesive systems, collagen shields, pseudolatices, and penetration enhancers. Ocular inserts provide sustained drug release and increased bioavailability. Evaluation methods for these systems include in vitro drug release and in vivo studies in animals.
This document discusses the qualification phases for manufacturing equipment validation: design qualification, installation qualification, operational qualification, and performance qualification. It provides details on the objectives and contents of documentation for each phase. Design qualification establishes the basic design criteria. Installation qualification verifies proper installation. Operational qualification tests functionality under normal operating conditions without product. Performance qualification demonstrates the equipment operates as intended under actual use conditions with product. Re-qualification is also discussed.
This document discusses in process quality control (IPQC) for various dosage forms. IPQC involves monitoring products during manufacturing to ensure quality and prevent errors. It includes tests of raw materials, in-process materials, and finished products. The objectives are to monitor features affecting quality and prevent errors. IPQC is required by FDA cGMP guidelines. Specific IPQC procedures are described for parenteral products, solid dosage forms, and semisolid dosage forms. Records of IPQC must be reviewed and batches released by quality control.
Validation (intro, scope, merits, ich, who guidelines)PRAJAKTASAWANT33
This document summarizes a presentation on validation given by Prajakta Sawant, a first year M.Pharm student at Alard College of Pharmacy in Pune, India. The presentation covered the need for validation, types of validation including process, cleaning, equipment and analytical method validation. It discussed validation concepts such as the validation master plan, documentation, and ICH and WHO guidelines. The goal of validation is to ensure consistent production of pharmaceuticals meeting quality standards.
Buccal Drug Delivery System Mali vv pptVidhyaMali1
BDDS refers to drug delivery systems that administer drugs through the buccal mucosa in the oral cavity. The buccal mucosa has a rich blood supply and provides a non-invasive route for systemic drug delivery with advantages like rapid absorption and avoidance of first-pass metabolism. Formulations can be designed as solids, semisolids, or liquids depending on the drug properties and desired release characteristics. The drug permeates through the buccal mucosa via transcellular or paracellular routes to enter systemic circulation. Buccal delivery offers an alternative to oral and parenteral routes for certain drugs.
This document discusses buccal drug delivery and mucoadhesion. It begins by covering topics like the introduction, classification of drug delivery in the oral mucosa (buccal vs sublingual delivery), anatomy of the buccal mucosa, principle of mucoadhesion and theories of mucoadhesion. It then discusses buccal drug delivery in more detail - including its applications, advantages, limitations and various buccal dosage forms. The key highlights are buccal drug delivery avoids first pass metabolism, maintains drug levels longer than sublingual route, and uses mucoadhesive polymers and dosage forms like patches, tablets and gels for drug retention in the buccal cavity.
Accelerated stability studies are conducted to increase the rate of chemical degradation or physical change of a drug product by using exaggerated storage conditions. The Arrhenius equation describes the dependence of the reaction rate constant on temperature and can be used to extrapolate accelerated stability data to long-term storage conditions. Types of accelerated stability tests include those at elevated temperatures, high intensity light, high partial pressure of oxygen, and high relative humidity. However, accelerated stability testing has limitations when degradation is caused by factors other than temperature, such as microbial contamination or diffusion, or when a product loses physical integrity at higher temperatures. International guidelines provide recommendations for conducting stress tests and evaluating stability data.
Pilot plant scale up for parenteral dosage formkoriyakrupali
The document discusses the scale-up of parenteral dosage forms from the laboratory to a pilot plant and full-scale production facility. A pilot plant is an intermediate facility that transforms a laboratory formula into a robust product through developing a reliable manufacturing method. This allows issues to be identified and addressed before full-scale production. The pilot plant is used to evaluate how the process may be affected by a large scale change and to produce trial lots for examination. It helps minimize waste and maximize yield of the prescribed dosage form.
This document discusses mucoadhesive drug delivery systems, specifically focusing on their use for buccal drug delivery. It begins with an introduction to mucoadhesion and bioadhesion. It then outlines the various routes mucoadhesive systems can be delivered through, including buccal, oral, vaginal, rectal, nasal and ocular delivery. The document focuses on the advantages of oral mucoadhesive systems for prolonged drug residence in the oral cavity. It discusses considerations for buccal drug delivery formulations, including drug properties, excipients used and factors affecting transmucosal permeability.
Gastro Retentive Drug Delivery system is a Novel drug delivery system which is more used to retain the drug for a longer period of time in the body and also to increase the GI transit time.
This document discusses modified release drug delivery systems (MRDDS), including extended release, delayed release, and targeted release dosage forms. It defines MRDDS as systems that control the time and location of drug release to accomplish therapeutic objectives. The document outlines the rationale for controlled drug delivery systems (CDDS), their advantages and disadvantages, criteria for selecting drug candidates, and important physiological and biological properties to consider for CDDS.
This document summarizes key concepts related to quality systems including change control, out of specifications, and out of trends. It defines change control as a procedure to review, verify, regulate, manage, approve and control changes made to existing systems or processes. It describes the process for managing change control including establishing written procedures and evaluating all changes that could impact quality, safety or efficacy. It also discusses out of specifications results as test results that fall outside established acceptance criteria and the procedures for investigating such results, including retesting and root cause analysis. Finally, it defines out of trend results as those that do not follow the expected trend over time and methods for identifying out of trend results.
This document discusses Good Manufacturing Practices (GMP) for pharmaceuticals. It introduces GMP, explaining that GMP ensures pharmaceutical products are consistently manufactured and controlled to quality standards for their intended use. It also discusses the relationships between quality assurance (QA), GMP, and quality control (QC), explaining that QA oversees the whole system, GMP is the quality system for manufacturing, and QC tests samples of products. Current good manufacturing practices (cGMP) are also introduced as the GMP regulations enforced by the FDA to control manufacturing operations and assure drug identity, strength, quality and purity.
This document discusses mucoadhesive drug delivery systems. It begins by defining mucoadhesive drug delivery as a system that utilizes the bioadhesive properties of water soluble polymers to target and maintain a drug at a specific site in the body for an extended period. It then describes several types of mucoadhesive systems including buccal, oral, nasal, rectal, and ocular. The document outlines the mechanism of mucoadhesion and factors affecting it. It evaluates various mucoadhesive dosage forms and concludes by discussing buccal drug delivery and its advantages and disadvantages.
This document discusses mucoadhesive drug delivery systems. It begins by defining bioadhesion and mucoadhesion, noting that mucoadhesion involves the attachment of a drug carrier to a mucosal surface like epithelial tissue. It then covers the concept of mucoadhesion in more detail and discusses the advantages and disadvantages of mucoadhesive drug delivery. Some key advantages include avoiding first pass metabolism, targeting drug delivery, and allowing delivery of drugs that are unstable in the stomach or intestines. The document also discusses the formulation design of mucoadhesive drug delivery systems.
Penetration Enhancers in Transdermal Drug Delivery SystemSimranDhiman12
Penetration Enhancers in Transdermal Drug Delivery System
Permeation enhancers are substances that reduce the skin barrier's ability to make skin more permeable and allow drug molecules to cross the skin at a faster rate
advantages and disadvantages
types of penetration enhancers
techniques
physical and chemical enhancers
Polymers with their use in pharmaceutics. Approaches in designing of control drug release delivery system. Classification of polymers according to their use in pharmacy field with their use in various use in dosage form development.
The Poisons Act of 1919 was passed to regulate and control the import, possession, and sale of poisons in India. The Act gives states the power to license and regulate the possession for sale and sale of specified poisons. It allows the regulation of import licenses for restricted poisons by the central government. Possession of poisons can be regulated in local areas where poisoning of cattle is common. Breach of the Act may result in fines or imprisonment. The Act categorizes poisons into two lists and provides some exemptions for substances in List B.
Introduction to Pharmaceutical Validation, Scope & Merits of Validation, Validation and calibration of Master plan, Hrs ICH & WHO guidelines for calibration and validation of
equipment's, Validation of specific dosage form, Types of validation. Government regulation, Manufacturing Process Model, URS, DQ, IQ, OQ & P.Q. of facilities.
Controlled Release Drug Delivery Systems - Types, Methods and ApplicationsSuraj Choudhary
This document discusses factors affecting the design of controlled release drug delivery systems (CRDDS). It outlines several key considerations for CRDDS design including selection of the drug candidate, medical and biological rationale, and physicochemical properties. It also discusses important physicochemical factors such as solubility, partition coefficient, molecular size and diffusivity, dose size, complexation, ionization constant, drug stability, and protein binding that influence CRDDS design. Finally, it briefly describes dissolution-controlled and diffusion-controlled release approaches for developing CRDDS.
Validation ensures that manufacturing systems, equipment, processes, and tests consistently produce quality products. It provides documented evidence that a process will reliably meet predetermined specifications. Validation studies are performed for analytical tests, equipment, facilities, and processes. Once validated, a system or process is expected to remain in control if unchanged; revalidation is required after modifications. Validation can be prospective, concurrent, retrospective, or through revalidation, and includes protocols for equipment, facilities, and manufacturing processes to demonstrate consistent performance under normal and worst-case conditions.
This document discusses the classification and types of stationary phases used in high performance liquid chromatography (HPLC). It classifies HPLC based on the type of elution used (isocratic or gradient) and based on the purpose and separation mechanism (partitioning, adsorption, ion exchange, size exclusion). It describes common stationary phases like silica, polymer, zirconia and monolithics. It also discusses bonded phases like C18, types of mobile phases used in normal phase, reverse phase, HILIC and ion pair chromatography.
This document provides an introduction to validation in the pharmaceutical industry. It discusses the origins and need for validation to ensure quality and control costs. The document outlines the key types of validation: prospective, retrospective, concurrent and revalidation. It also describes the scope of validation, noting it requires appropriate infrastructure, documentation, personnel and management involvement. Validation should be performed for facilities, equipment, utilities, processes and when major changes occur to demonstrate consistency in producing products that meet specifications.
The document discusses drug delivery through the nasal and pulmonary routes. It begins by describing the anatomy of the nose and lungs. It then discusses various nasal and pulmonary drug delivery systems including liquid and solid dosage forms for nasal delivery as well as metered dose inhalers, dry powder inhalers, and nebulizers for pulmonary delivery. Finally, it outlines some advantages of these routes such as rapid drug absorption, avoidance of first-pass metabolism, and lower dosing requirements.
Approaches to extend gastro intestine transitPragatitrivedi2
This document discusses various approaches to extend gastrointestinal transit time, including gastroretentive drug delivery systems (GRDDS). It describes 7 main approaches: 1) floating drug delivery systems, 2) mucoadhesive systems, 3) raft-forming systems, 4) low density systems, 5) expandable or unfoldable systems, 6) swellable systems, and 7) super porous hydrogels. Each approach aims to prolong the retention time of drugs in the stomach to allow for extended release of drugs that are best absorbed in the upper gastrointestinal tract.
Liposomes and liposomal drug delivery system( recent advancement)Unmesh Bhamare
This document summarizes a seminar presentation on recent trends in pharmaceutical sciences focusing on liposomes. It defines liposomes as concentric bilayered vesicles enclosing an aqueous volume within a phospholipid membrane. The presentation covers the structural components of liposomes including commonly used phospholipids, classification based on lamellarity and size, various preparation methods such as mechanical dispersion, solvent dispersion, and detergent removal. It also discusses characterization, stability considerations, applications in drug delivery, recent advances, and some marketed liposome products.
This document provides an overview of liposomes, including their composition, advantages, classification, preparation methods, characterization, and applications. Liposomes are spherical vesicles composed of phospholipid bilayers that can encapsulate drugs. They range in size from 20nm to several micrometers. Key advantages include biodegradability, protection of encapsulated drugs, and improved drug pharmacokinetics. Common preparation methods include mechanical dispersion, solvent dispersion, and detergent removal. Liposomes are characterized based on size, surface charge, drug entrapment percentage, and lamellarity. They have applications as drug and gene delivery vehicles in cancer therapy, antimicrobial therapy, and more.
Accelerated stability studies are conducted to increase the rate of chemical degradation or physical change of a drug product by using exaggerated storage conditions. The Arrhenius equation describes the dependence of the reaction rate constant on temperature and can be used to extrapolate accelerated stability data to long-term storage conditions. Types of accelerated stability tests include those at elevated temperatures, high intensity light, high partial pressure of oxygen, and high relative humidity. However, accelerated stability testing has limitations when degradation is caused by factors other than temperature, such as microbial contamination or diffusion, or when a product loses physical integrity at higher temperatures. International guidelines provide recommendations for conducting stress tests and evaluating stability data.
Pilot plant scale up for parenteral dosage formkoriyakrupali
The document discusses the scale-up of parenteral dosage forms from the laboratory to a pilot plant and full-scale production facility. A pilot plant is an intermediate facility that transforms a laboratory formula into a robust product through developing a reliable manufacturing method. This allows issues to be identified and addressed before full-scale production. The pilot plant is used to evaluate how the process may be affected by a large scale change and to produce trial lots for examination. It helps minimize waste and maximize yield of the prescribed dosage form.
This document discusses mucoadhesive drug delivery systems, specifically focusing on their use for buccal drug delivery. It begins with an introduction to mucoadhesion and bioadhesion. It then outlines the various routes mucoadhesive systems can be delivered through, including buccal, oral, vaginal, rectal, nasal and ocular delivery. The document focuses on the advantages of oral mucoadhesive systems for prolonged drug residence in the oral cavity. It discusses considerations for buccal drug delivery formulations, including drug properties, excipients used and factors affecting transmucosal permeability.
Gastro Retentive Drug Delivery system is a Novel drug delivery system which is more used to retain the drug for a longer period of time in the body and also to increase the GI transit time.
This document discusses modified release drug delivery systems (MRDDS), including extended release, delayed release, and targeted release dosage forms. It defines MRDDS as systems that control the time and location of drug release to accomplish therapeutic objectives. The document outlines the rationale for controlled drug delivery systems (CDDS), their advantages and disadvantages, criteria for selecting drug candidates, and important physiological and biological properties to consider for CDDS.
This document summarizes key concepts related to quality systems including change control, out of specifications, and out of trends. It defines change control as a procedure to review, verify, regulate, manage, approve and control changes made to existing systems or processes. It describes the process for managing change control including establishing written procedures and evaluating all changes that could impact quality, safety or efficacy. It also discusses out of specifications results as test results that fall outside established acceptance criteria and the procedures for investigating such results, including retesting and root cause analysis. Finally, it defines out of trend results as those that do not follow the expected trend over time and methods for identifying out of trend results.
This document discusses Good Manufacturing Practices (GMP) for pharmaceuticals. It introduces GMP, explaining that GMP ensures pharmaceutical products are consistently manufactured and controlled to quality standards for their intended use. It also discusses the relationships between quality assurance (QA), GMP, and quality control (QC), explaining that QA oversees the whole system, GMP is the quality system for manufacturing, and QC tests samples of products. Current good manufacturing practices (cGMP) are also introduced as the GMP regulations enforced by the FDA to control manufacturing operations and assure drug identity, strength, quality and purity.
This document discusses mucoadhesive drug delivery systems. It begins by defining mucoadhesive drug delivery as a system that utilizes the bioadhesive properties of water soluble polymers to target and maintain a drug at a specific site in the body for an extended period. It then describes several types of mucoadhesive systems including buccal, oral, nasal, rectal, and ocular. The document outlines the mechanism of mucoadhesion and factors affecting it. It evaluates various mucoadhesive dosage forms and concludes by discussing buccal drug delivery and its advantages and disadvantages.
This document discusses mucoadhesive drug delivery systems. It begins by defining bioadhesion and mucoadhesion, noting that mucoadhesion involves the attachment of a drug carrier to a mucosal surface like epithelial tissue. It then covers the concept of mucoadhesion in more detail and discusses the advantages and disadvantages of mucoadhesive drug delivery. Some key advantages include avoiding first pass metabolism, targeting drug delivery, and allowing delivery of drugs that are unstable in the stomach or intestines. The document also discusses the formulation design of mucoadhesive drug delivery systems.
Penetration Enhancers in Transdermal Drug Delivery SystemSimranDhiman12
Penetration Enhancers in Transdermal Drug Delivery System
Permeation enhancers are substances that reduce the skin barrier's ability to make skin more permeable and allow drug molecules to cross the skin at a faster rate
advantages and disadvantages
types of penetration enhancers
techniques
physical and chemical enhancers
Polymers with their use in pharmaceutics. Approaches in designing of control drug release delivery system. Classification of polymers according to their use in pharmacy field with their use in various use in dosage form development.
The Poisons Act of 1919 was passed to regulate and control the import, possession, and sale of poisons in India. The Act gives states the power to license and regulate the possession for sale and sale of specified poisons. It allows the regulation of import licenses for restricted poisons by the central government. Possession of poisons can be regulated in local areas where poisoning of cattle is common. Breach of the Act may result in fines or imprisonment. The Act categorizes poisons into two lists and provides some exemptions for substances in List B.
Introduction to Pharmaceutical Validation, Scope & Merits of Validation, Validation and calibration of Master plan, Hrs ICH & WHO guidelines for calibration and validation of
equipment's, Validation of specific dosage form, Types of validation. Government regulation, Manufacturing Process Model, URS, DQ, IQ, OQ & P.Q. of facilities.
Controlled Release Drug Delivery Systems - Types, Methods and ApplicationsSuraj Choudhary
This document discusses factors affecting the design of controlled release drug delivery systems (CRDDS). It outlines several key considerations for CRDDS design including selection of the drug candidate, medical and biological rationale, and physicochemical properties. It also discusses important physicochemical factors such as solubility, partition coefficient, molecular size and diffusivity, dose size, complexation, ionization constant, drug stability, and protein binding that influence CRDDS design. Finally, it briefly describes dissolution-controlled and diffusion-controlled release approaches for developing CRDDS.
Validation ensures that manufacturing systems, equipment, processes, and tests consistently produce quality products. It provides documented evidence that a process will reliably meet predetermined specifications. Validation studies are performed for analytical tests, equipment, facilities, and processes. Once validated, a system or process is expected to remain in control if unchanged; revalidation is required after modifications. Validation can be prospective, concurrent, retrospective, or through revalidation, and includes protocols for equipment, facilities, and manufacturing processes to demonstrate consistent performance under normal and worst-case conditions.
This document discusses the classification and types of stationary phases used in high performance liquid chromatography (HPLC). It classifies HPLC based on the type of elution used (isocratic or gradient) and based on the purpose and separation mechanism (partitioning, adsorption, ion exchange, size exclusion). It describes common stationary phases like silica, polymer, zirconia and monolithics. It also discusses bonded phases like C18, types of mobile phases used in normal phase, reverse phase, HILIC and ion pair chromatography.
This document provides an introduction to validation in the pharmaceutical industry. It discusses the origins and need for validation to ensure quality and control costs. The document outlines the key types of validation: prospective, retrospective, concurrent and revalidation. It also describes the scope of validation, noting it requires appropriate infrastructure, documentation, personnel and management involvement. Validation should be performed for facilities, equipment, utilities, processes and when major changes occur to demonstrate consistency in producing products that meet specifications.
The document discusses drug delivery through the nasal and pulmonary routes. It begins by describing the anatomy of the nose and lungs. It then discusses various nasal and pulmonary drug delivery systems including liquid and solid dosage forms for nasal delivery as well as metered dose inhalers, dry powder inhalers, and nebulizers for pulmonary delivery. Finally, it outlines some advantages of these routes such as rapid drug absorption, avoidance of first-pass metabolism, and lower dosing requirements.
Approaches to extend gastro intestine transitPragatitrivedi2
This document discusses various approaches to extend gastrointestinal transit time, including gastroretentive drug delivery systems (GRDDS). It describes 7 main approaches: 1) floating drug delivery systems, 2) mucoadhesive systems, 3) raft-forming systems, 4) low density systems, 5) expandable or unfoldable systems, 6) swellable systems, and 7) super porous hydrogels. Each approach aims to prolong the retention time of drugs in the stomach to allow for extended release of drugs that are best absorbed in the upper gastrointestinal tract.
Liposomes and liposomal drug delivery system( recent advancement)Unmesh Bhamare
This document summarizes a seminar presentation on recent trends in pharmaceutical sciences focusing on liposomes. It defines liposomes as concentric bilayered vesicles enclosing an aqueous volume within a phospholipid membrane. The presentation covers the structural components of liposomes including commonly used phospholipids, classification based on lamellarity and size, various preparation methods such as mechanical dispersion, solvent dispersion, and detergent removal. It also discusses characterization, stability considerations, applications in drug delivery, recent advances, and some marketed liposome products.
This document provides an overview of liposomes, including their composition, advantages, classification, preparation methods, characterization, and applications. Liposomes are spherical vesicles composed of phospholipid bilayers that can encapsulate drugs. They range in size from 20nm to several micrometers. Key advantages include biodegradability, protection of encapsulated drugs, and improved drug pharmacokinetics. Common preparation methods include mechanical dispersion, solvent dispersion, and detergent removal. Liposomes are characterized based on size, surface charge, drug entrapment percentage, and lamellarity. They have applications as drug and gene delivery vehicles in cancer therapy, antimicrobial therapy, and more.
1. Liposomes are spherical vesicles made of phospholipid bilayers that can encapsulate aqueous content. They range in size from 20nm to micrometers.
2. Liposomes are composed mainly of phospholipids and cholesterol. Commonly used phospholipids include phosphatidylcholine, phosphatidylethanolamine, and dioleoyl phosphatidylcholine. Cholesterol helps stabilize the bilayer structure.
3. Liposomes offer advantages like low toxicity, biodegradability, protection of encapsulated drugs, and improved pharmacokinetics. However, they also have disadvantages such as drug leakage, short half-life, high production costs, and difficulty in large-scale manufacturing
This document discusses liposomes, which are spherical vesicles made of phospholipids that can encapsulate drugs. It covers the mechanism of liposome formation, types of phospholipids used, methods of preparation, characterization, and applications. Liposomes can be used to deliver drugs to target sites and prolong drug circulation time, reducing side effects. They show potential for targeted delivery of anticancer drugs, vaccines, and other therapeutics.
This document summarizes a seminar presentation on liposomes and niosomes. It discusses various types of liposomes and methods for preparing liposomes, including solvent dispersion methods like ethanol injection, ether injection, and reverse phase evaporation. Characterization techniques for liposomes like size, shape, encapsulation efficiency, and drug release are also outlined. Finally, the document notes therapeutic applications of liposomes for drug delivery and discusses characterization of liposomes through parameters like vesicle shape, size, surface charge, and drug entrapment efficiency.
This document discusses various techniques for preparing and characterizing liposomes. It describes common methods for passive loading of drugs into liposomes, such as freeze drying, ethanol injection, ether injection, and reverse-phase evaporation. It also discusses remote loading using pH gradients or electrical potentials. Characterization techniques discussed include measuring particle size, surface charge, drug encapsulation efficiency, transition temperature, and drug release rate. Methods are provided for determining important chemical characteristics like phospholipid and cholesterol content.
This document discusses liposomal drug delivery systems. It begins by defining liposomes as bilayered vesicles composed of phospholipids that can encapsulate aqueous cores. Liposomes range in size from 20nm to several micrometers. The document then outlines the advantages of liposomal drug delivery such as improved targeting, controlled release, and reduced toxicity. Several methods for preparing and loading liposomes are also described. The document concludes by discussing some applications of liposomal drug delivery including cancer therapy, antimicrobial treatments, and gene delivery.
This document provides an overview of liposomes as a drug delivery system. It begins by defining liposomes as spherical vesicles composed of lipid bilayers that can encapsulate aqueous volumes. Liposomes were first produced in 1961. The document then discusses the composition of liposomes, including phospholipids and cholesterol as main components. It describes various methods for liposome preparation, such as film hydration, sonication, extrusion, and detergent removal. Characterization techniques are also outlined. In summary, this document introduces liposomes as lipid bilayer structures for drug delivery and encapsulation, and covers their composition, methods of preparation, and characterization.
Liposomes are spherical vesicles made of phospholipid bilayers that can encapsulate hydrophilic or hydrophobic drugs. They range in size from 25nm to 5000nm. This document discusses the structure of liposomes and their components, including phospholipids and cholesterol. Various preparation methods are described, such as lipid film hydration, ethanol injection, and detergent removal. Liposomes offer advantages for drug delivery, such as the ability to encapsulate different drug types and provide controlled release. They can be classified based on structure, method of preparation, composition, and specialty type.
Liposomes are spherical vesicles made of phospholipid bilayers that can encapsulate drugs for delivery. They range in size from 25nm to 5000nm. Liposomes are prepared through methods like lipid film hydration, microemulsification, sonication, or membrane extrusion. They offer advantages for delivering both hydrophobic and hydrophilic drugs and allow for controlled release. Liposomes can be classified based on their structure, preparation method, composition, and application.
Liposomes are spherical vesicles made of phospholipid bilayers that can encapsulate hydrophilic or hydrophobic drugs. They range in size from 25nm to 5000nm. This document discusses the structure of liposomes and their components, including phospholipids and cholesterol. It also covers various preparation methods such as lipid film hydration, extrusion, and detergent removal. Liposomes offer advantages for drug delivery such as the ability to encapsulate different drug types and provide controlled release, but also have challenges like high production costs and drug leakage.
Liposomes are spherical vesicles composed of phospholipid bilayers that can encapsulate water-soluble drugs in their aqueous core and lipid-soluble drugs within their membrane. They have advantages for drug delivery such as providing selective targeting to tissues, increasing drug efficacy and stability, and reducing toxicity. However, they also have challenges with drug leakage and uptake by the reticuloendothelial system. Liposomes can be classified based on their lamellarity and size, and are prepared using methods like film hydration, ethanol injection, and detergent removal. They have applications for delivery of drugs, genes, vaccines, and contrast agents for imaging.
Liposomes are spherical vesicles composed of lipid bilayers that can encapsulate aqueous content. They are used as drug delivery systems to improve drug solubility, stability, and targeting. Liposomes are prepared using various methods involving dispersion of lipids in aqueous solution. Key components are phospholipids like phosphatidylcholine and cholesterol. Characterization evaluates parameters like size, shape, drug entrapment efficiency, and phase behavior. Liposomes offer benefits like increased drug efficacy and stability but also have challenges like short shelf life and high production costs.
Niosomes are novel drug delivery systems composed of non-ionic surfactants and cholesterol. They can encapsulate both hydrophilic and lipophilic drugs. Niosomes are prepared using methods like ether injection, film hydration, sonication, and microfluidization. Key factors that affect niosome formation include the surfactant used, addition of cholesterol, and hydration temperature. Niosomes offer advantages over liposomes like improved stability and the ability to entrap both hydrophilic and hydrophobic drugs. Niosomes find applications in targeted drug delivery through routes like transdermal, parenteral, oral and for ophthalmic and radiopharmaceutical uses.
This document discusses vesicular drug delivery systems (VDDS), including their classification, advantages, and formulation methods. It summarizes that VDDS can be classified as lipoidal or non-lipoidal carriers, with liposomal systems like liposomes, ethosomes, transfersomes discussed in detail. The advantages of VDDS include effective drug permeation, prolonged circulation time, reduced toxicity and cost of therapy. However, VDDS also have disadvantages like low drug loading efficiency and stability issues. The document provides an overview of various vesicular carrier preparation techniques for developing novel drug delivery systems.
1. Liposomes are spherical vesicles made of concentric phospholipid bilayers that can encapsulate aqueous solutions. They form spontaneously when phospholipids are exposed to aqueous solutions.
2. Liposomes have many advantages for drug delivery such as increased drug efficacy, stability, and targeting to tumor tissues while reducing toxicity. However, they also have disadvantages like high production costs, drug leakage, and short half-life.
3. There are various methods for preparing and loading drugs into liposomes, including mechanical dispersion techniques using sonication or extrusion to reduce liposome size, and solvent dispersion techniques using thin film hydration. Characterization and stability testing of the liposomes is important.
Liposomes are spherical vesicles made of lipid bilayers that can encapsulate aqueous content. They structurally consist of concentric bilayers surrounding an inner aqueous volume. This allows both hydrophilic drugs in the inner volume and hydrophobic drugs in the bilayer. Liposomes offer advantages like increased drug efficacy, reduced toxicity, and passive tumor targeting. However, developing stable liposomal formulations at an industrial scale can be difficult due to physical and chemical instability issues. Niosomes are similar non-ionic surfactant based vesicles that offer many of the same advantages as liposomes while being more stable and less toxic.
This document provides an overview of niosomes, which are non-ionic surfactant vesicles that can be used as drug carriers. It discusses the structure of niosomes, how they are formulated using various methods, and how the formulations are characterized. It also outlines the advantages of niosomes over liposomes as a drug delivery system. Some therapeutic applications of niosomes are described, such as for cancer treatment, mitochondrial disorders, and leishmaniasis therapy. Finally, examples of specific drugs that have been formulated into niosomes are listed.
Liposomal drug delivery involves encapsulating drugs within liposomes, which are spherical vesicles composed of phospholipid bilayers, to improve drug targeting and reduce toxicity. Liposomes can be classified based on lamellarity, size, and method of preparation. Drugs are encapsulated within the aqueous interior or phospholipid bilayer of liposomes. Liposomes protect drugs, control drug release, and can be targeted to specific tissues. Applications include cancer therapy, antimicrobial delivery, ophthalmic delivery, and topical delivery to improve treatment.
Downstreamprocessing of Cephalosporins and Aspartic acidSurender Rawat
This document discusses the production and purification of L-aspartic acid through fermentation. Key points:
- L-aspartic acid is produced from ammonium fumarate by fermentation using immobilized E. coli cells. It is one of the most commonly produced amino acids, with an annual production of 4000 metric tons.
- Downstream processing involves centrifugation to remove cells, followed by precipitation of aspartic acid at its isoelectric point of pH 2.7 using a glycine buffer. Further purification steps include chromatography techniques like HPLC and ion exchange chromatography.
- Final purification is done via cation exchange chromatography using an SP Sepharose column, eluting the aspartic
Similar to Liposomes 141009105743-conversion-gate02 (20)
3. LIPOSOMES:
Liposomes are cocentric bilayered
vesicles in which an aqueous
volume is entirely enclosed by
a membranous lipid bilayer mainly
composed of natural or
synthetic phospholipids.
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4. • Liposomes were discovered about 40 years ago by Alec
Bingham.
• Liposomes can be produced from cholesterols, non toxic
surfactants,sphingolipids,glycolipids,long chain fatty acids &
even membrane proteins.
• Liposomes are the drug carrier loaded with great variety of
molecules such as small drug molecules, proteins,
nucleotides & even plasmids.
• Considerable progress was made during 1970s and 1980s in
the field of liposome stability leading to long circulation
times of liposomes
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7. • Phospholipids are major structural components of
biological membranes in human body, where 2 types of
phospholipids exist i.e. phosphodiglycerides &
sphingolipids .
• Each phospholipid molecule has 3 major parts, 1 head & 2
tails. Head is made from 3 molecular components: choline ,
phosphate & glycerol which is hydrophilic.Each tail with a
long chain EFA which are hydrophobic.
• Most commonly used phospholipids – PC an amphipathic
molecule with a hydrophilic polar head group,
phosphocholine . PC, also known as “lecithin”, can be
derived from natural and synthetic sources.
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8. The lipid bi-layer used in the liposomes are usually made of
phospholipids and cholesterol.
Following are the
A) Naturally occurring phospholipids used in liposomes are:
• Phosphatidylcholine (PC),
• Phosphatidylethanolamine (PE),
• Phosphatidylserine (PS).
B) Synthetic phospholipids used in the liposomes are:
• Dioleoyl phosphatidylcholine (DOPC),
• Distearoyl phosphatidylcholine (DSPC),
• Dioleoyl phosphatidylethanolamine (DOPE),
• Distearoyl phosphatidylethanolamine (DSPE).
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9. CLASSIFICATION:
VESICLE TYPE ABBREVIATI
ON
DIAMETER
SIZE
NO. OF LIPID BI -
LAYER
Unilamellar vesicle UV All size range ONE
Small unilamellar vesicle SUV 20-100 nm ONE
Medium unilamellar vesicle MUV >100μm ONE
Large unilamellar vesicle LUV >1000μm ONE
Giant unilamellar vesicle GUV >1μm ONE
Oligolamellar vesicle OLV 0.1-1μm 5
Multilamellar vesicle MLV >0.5μm 5-25
Multivesicular vesicle MV >1μm Multicompartmental
structure
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10. FORMATION OF LIPOSOME:
When phospholipids are
dispersed in water, they
spontaneously form closed
structure with internal aqueous
environment bounded by
phospholipid bilayer membranes,
this vesicular system is called as
liposome.
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15. BATH SONICATOR PROBE SONICATOR
1.Large volume of diluted lipids are
processed.
1.Small volume of diluted lipids are
processed.
2.Less or no contamination. 2.Chances of contamination.
• At high energy levels, average size of vesicles is further
reduced.
• Exposure of MLV’s to ultrasonic irradiations is the most
widely used method for producing small vesicles.
• As chances of contamination are likely to occur in probe
sonicator, bath sonicator is widely used.
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16. II) FRENCH PRESSURE CELLS(ULV/OLV):
• Method developed by Barenholtz & Hamilton et al.
• Very useful method in which extrusion of preformed large
liposomes in a French Pressure under very high pressure is
carried out .
• This technique yields ULV’s/OLV’s of intermediate size(30-
80nm/depending upon applied pressure).
• Liposomes are more stable.
• Free from structural defects.
• Leakage problem is also less.
• However it has high production cost. 16
17. III) FREEZE THAW SONICATION(FTS):
Freeze SUV dispersion
thaw at room temperature for 15 minutes
sonicate
rupture of SUV’s occur
Formation of liposomes
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18. SOLVENT DISPERSION METHODS
I) ETHANOL INJECTION METHOD
Lipids ethanol
Rapidly inject through a fine needle
Saline buffer containing materials to be entrapped
dissolution of ethanol
Formation of SUV’s.
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19. II) ETHER INJECTION METHOD:
Lipid ether
slowly injecting through a narrow needle
vapourize temperature at 60˚C
production of SUV’s.
• Less risk of oxidation as ether is free of peroxides.
• Low efficiency.
• Long time needed for production. 19
20. REVERSE PHASE EVAPORATION VESICLES
Lipid organic solvent aqueous solution
mix
sonicate
formation of w/o emulsion
evaporate to remove the organic solvent
Lipids form a phospholipid bilayer
vigorous shaking
water droplets collapse
formation of LUV’s.
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21. CHARACTERIZATION:
PARTICLE SIZE ANALYSIS-
• Laser light scattering, transmission electron microscopy
determines the particle size & its distribution.
SURFACE CHARGE-
• Free-flow electrophoresis on a cellulose acetate plate in a sodium
borate buffer pH 8.8 & a zeta potential measurement.
• The samples are applied to plate & electrophoresis is carried out
at 4˚C for 30 min.
• The plate is dried and phospholipids are visualised by the
molybdenum blue reagent.
• The liposomes get bifurcated based on the surface charge.
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22. PERCENT DRUG ENTRAPMENT-This
can be determined by ‘PROTAMINE AGGREGATE’ &
‘MINICOLUMN CENTRIFUGATION method . Expressed as
%entrapment/mg lipid.
PHASE BEHAVIOUR-Liposomes
at transition temperature undergo reversible
phase transition i.e the polar head groups in gel state become
disordered to form the liquid crystalline state which can be
determined by DSC.
LAMELLARITY-Freeze-
fracture electron microscopy & freeze-etch electron
microscopy & P-NMR method.
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23. STABILITY OF LIPOSOMES:
A. PREVENTION OF CHEMICAL DEGRADATION:
1.Start with freshly purified lipids & freshly distilled solvents.
2.Avoid procedure which involving high temperature.
3.Carry out manufacturing in the absence of oxygen.
4.Deoxygenate aqueous solution with nitrogen.
5.Store liposome suspension in an inert atmosphere.
6.Include an antioxidant as a component.
7.Iron chelater is used to prevent initiation of free radical
chain reaction.
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24. B. PREVENTION OF PHYSICAL DEGRADATION:
1.‘ANNEALING’ is best method to control physical degradation
i.e incubating the liposomes at a temperature high enough
above the phase transition temperature to allow differences in
packing density between opposite sides of the bilayers to
equalize by trans membrane flip-flop .
2. The stability of liposomes may also be increased by cross
linking membrane component covalently using Gluteraldehyde
fixation, osmification or polymerization of alkyne containing
phospholipids. These methods increases mechanical strength
of the membrane & render them less susceptible to disruption.
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25. APPLICATIONS:
1.The therapeutic value of liposomes as drug carriers,
particularly for anticancer, antifungal, and antibacterial
agents.
2.As anticancer , cytotoxic drugs like Cytarabine, alkylating
agents .
3.As vaccine adjuvants i.e. when administered by IM route,
they slowly release the antigens and accumulate in lymph
nodes.
4.In ophthalmic drug delivery systems,Idoxuridine used in
acute & chronic keratitis . 25
26. 5. Sustained release system of systemically or locally
administered liposomes. Ex biological proteins or peptides
such as vasopressin.
6. Site specific targeting: in certain cases liposomes with
surface attached ligands can bind to target cells (‘key and
lock’ mechanism). Ex antineos, anti infectors &
antiinflammatory drugs.
7. Improved transfer of hydrophilic, charged molecules like
chelators , antibiotics, plasmids & genes into the cells.
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27. RECENT ADVANCES & ON GOING
CLINICAL TRIALS:
Antigens as Liposomal Preparation Applications:
• Diphtheria toxoid = Superior immunoadjuvant
• Herpes simplex virus = Enhanced Ab level
• Hepatitis B virus = Higher Ab response
• Bacterial polysaccharides = Superior immunoadjuvants
Tetanus toxoids = Increased Ab titre
• Influenza subunit antigen = Intranasal, protects animal
from virus
• Carbohydrate antigen = Increased Ab titre in salivary
gland
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