This document summarizes a seminar presentation on microspheres as a novel drug delivery system. It discusses the needs for microspheres, their ideal characteristics, advantages and disadvantages. It also outlines different methods for preparing microspheres, including solvent evaporation, hot melt microencapsulation, solvent extraction, hydrogel microspheres, and spray drying. The document provides details on the materials and evaluation of microspheres and their applications in marketed formulations.
Microspheres Preparation and Evaluations.pptxRAHUL PAL
This document discusses microspheres, including their definition, classification, preparation methods, evaluation, applications, and marketed preparations. Microspheres are spherical particles between 1-1000 μm in size that can be made of polymers, proteins, or synthetic materials. Common preparation methods include single/double emulsion, solvent evaporation, phase separation coacervation, spray drying, and polymerization. Microspheres are evaluated based on particle size, drug entrapment efficiency, swelling index, and in vitro drug release. They have applications in oral, nasal, ocular, and transdermal drug delivery due to their ability to provide sustained release and target drug delivery.
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.
Microspheres are solid spherical particles ranging in size from 1-1000μm that can be used for drug delivery. They provide advantages like constant drug release, reduced dosing, and protection of drugs from degradation. Microspheres are made of polymers and exist as microcapsules or micromatrices. Various preparation methods include solvent evaporation, single/double emulsion, and polymerization. Microspheres find applications in oral, nasal, ocular, and other localized drug deliveries due to their ability to target tissues and control drug release kinetics.
Niosomes are non-ionic surfactant-based vesicles that can encapsulate aqueous solutions within a bilayer membrane. There are three types - small unilamellar vesicles, large unilamellar vesicles, and multi-lamellar vesicles. Niosomes can be used for controlled drug release, to improve drug stability and bioavailability, and for targeting drugs to specific sites in the body like the liver or tumors. They have applications in delivery of drugs, vaccines, hemoglobin, and cosmetic agents to the skin.
AQUASOMES: A NOVEL CARRIER FOR DRUG DELIVERY SYSTEMMUSTAFIZUR RAHMAN
This document discusses aquasomes, which are spherical nanoparticle carrier systems composed of a solid nanocrystalline core coated with an oligomeric film. Aquasomes are self-assembled using non-covalent and ionic bonds. They are used to deliver and protect delicate biomolecules. The core provides structural stability while the carbohydrate coating protects against dehydration and stabilizes biomolecules. Common methods to prepare aquasomes include precipitating a ceramic core, coating it with disaccharides using sonication, and immobilizing a drug molecule onto the coated particles. Potential applications of aquasomes include insulin delivery, oral enzyme delivery, oxygen transport, antigen delivery, and drug or gene delivery.
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.
Microspheres are solid spherical particles made of polymers that can encapsulate drugs. They range in size from 1-1000μm. There are various methods for producing microspheres, including single and double emulsion techniques, polymerization methods, coacervation, spray drying, and solvent extraction. Microspheres offer advantages like controlled drug release, protection of unstable drugs, and targeting of specific tissues. They have various pharmaceutical applications including vaccine and drug delivery, with the ability to control release kinetics and target specific sites.
This document discusses mechanical and pH activated drug delivery systems. Mechanical systems include metered dose inhalers, dry powder inhalers, and nebulizers which deliver drugs through physical activation. pH activated systems target drug delivery based on pH ranges in different body regions. They are classified as hydrogels, nanoparticles, microspheres, and microgels which protect drugs from gastric conditions and release them in the intestines based on pH changes. The advantages are site-specific delivery and protection of drugs, while disadvantages include non-biodegradability of polymers and lack of specificity between similar pH regions.
Microspheres Preparation and Evaluations.pptxRAHUL PAL
This document discusses microspheres, including their definition, classification, preparation methods, evaluation, applications, and marketed preparations. Microspheres are spherical particles between 1-1000 μm in size that can be made of polymers, proteins, or synthetic materials. Common preparation methods include single/double emulsion, solvent evaporation, phase separation coacervation, spray drying, and polymerization. Microspheres are evaluated based on particle size, drug entrapment efficiency, swelling index, and in vitro drug release. They have applications in oral, nasal, ocular, and transdermal drug delivery due to their ability to provide sustained release and target drug delivery.
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.
Microspheres are solid spherical particles ranging in size from 1-1000μm that can be used for drug delivery. They provide advantages like constant drug release, reduced dosing, and protection of drugs from degradation. Microspheres are made of polymers and exist as microcapsules or micromatrices. Various preparation methods include solvent evaporation, single/double emulsion, and polymerization. Microspheres find applications in oral, nasal, ocular, and other localized drug deliveries due to their ability to target tissues and control drug release kinetics.
Niosomes are non-ionic surfactant-based vesicles that can encapsulate aqueous solutions within a bilayer membrane. There are three types - small unilamellar vesicles, large unilamellar vesicles, and multi-lamellar vesicles. Niosomes can be used for controlled drug release, to improve drug stability and bioavailability, and for targeting drugs to specific sites in the body like the liver or tumors. They have applications in delivery of drugs, vaccines, hemoglobin, and cosmetic agents to the skin.
AQUASOMES: A NOVEL CARRIER FOR DRUG DELIVERY SYSTEMMUSTAFIZUR RAHMAN
This document discusses aquasomes, which are spherical nanoparticle carrier systems composed of a solid nanocrystalline core coated with an oligomeric film. Aquasomes are self-assembled using non-covalent and ionic bonds. They are used to deliver and protect delicate biomolecules. The core provides structural stability while the carbohydrate coating protects against dehydration and stabilizes biomolecules. Common methods to prepare aquasomes include precipitating a ceramic core, coating it with disaccharides using sonication, and immobilizing a drug molecule onto the coated particles. Potential applications of aquasomes include insulin delivery, oral enzyme delivery, oxygen transport, antigen delivery, and drug or gene delivery.
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.
Microspheres are solid spherical particles made of polymers that can encapsulate drugs. They range in size from 1-1000μm. There are various methods for producing microspheres, including single and double emulsion techniques, polymerization methods, coacervation, spray drying, and solvent extraction. Microspheres offer advantages like controlled drug release, protection of unstable drugs, and targeting of specific tissues. They have various pharmaceutical applications including vaccine and drug delivery, with the ability to control release kinetics and target specific sites.
This document discusses mechanical and pH activated drug delivery systems. Mechanical systems include metered dose inhalers, dry powder inhalers, and nebulizers which deliver drugs through physical activation. pH activated systems target drug delivery based on pH ranges in different body regions. They are classified as hydrogels, nanoparticles, microspheres, and microgels which protect drugs from gastric conditions and release them in the intestines based on pH changes. The advantages are site-specific delivery and protection of drugs, while disadvantages include non-biodegradability of polymers and lack of specificity between similar pH regions.
This document discusses microcapsules and microspheres, including their types, sizes, materials used, and preparation methods. Microcapsules contain an active agent surrounded by a polymeric shell, while microspheres are small spherical particles made of polymers, glass, or ceramics between 1-1000 microns in diameter. Common preparation methods include emulsion polymerization, interfacial polycondensation, suspension crosslinking, solvent evaporation/extraction, and coacervation/phase separation.
Microspheres and microcapsules are spherical particles ranging from 1 μm to 1000 μm in diameter that can be used to encapsulate drugs for controlled release. Microspheres contain drug distributed throughout while microcapsules contain drug enclosed within a coating. Various natural and synthetic polymers are used to prepare microspheres and microcapsules through techniques like solvent evaporation, emulsion polymerization, and coacervation. Microspheres and microcapsules offer benefits like sustained drug release, targeted drug delivery, and reduced dosing frequency. They are evaluated based on particle size, drug entrapment efficiency, in vitro drug release, and other physicochemical properties.
This document discusses various analytical techniques used to evaluate protein and peptide drug formulations, including stability testing, bioassays, UV spectroscopy, Bradford assay, differential scanning calorimetry, chromatography, and electrophoresis. Stability testing evaluates how environmental factors affect the quality of a drug over time. Bioassays assess potency by monitoring the in vitro or in vivo pharmacological response to the protein. UV spectroscopy, Bradford assay, and electrophoresis can be used to detect and quantify the amount of protein present in a sample. Chromatography and differential scanning calorimetry provide information about stability and conformational changes of proteins.
Protein and-peptide-drug-delivery-systemsGaurav Kr
The document discusses protein and peptide drug delivery systems. It begins by defining proteins and peptides, noting that proteins are molecules composed of over 50 amino acids, while peptides are molecules composed of less than 50 amino acids. It then discusses how scientific advances in molecular and cell biology have led to the development of recombinant DNA and hybridoma technology to produce protein products. The document provides examples of marketed protein and peptide drugs and discusses challenges with delivering these drugs orally due to their large molecular size and susceptibility to enzymatic degradation. It explores approaches to protein and peptide delivery including non-parenteral systemic delivery methods and various considerations for developing delivery systems for these pharmaceuticals.
Content:
Introduction
Ideal Properties
Advantages
Limitations
Types of Microsphere
Method for Preparation
Polymer Used for Preparation
Release of Drug from Microsphere
Application
This document provides an overview of protein and peptide drug delivery. It begins with definitions of proteins and peptides and descriptions of protein structure. It then discusses protein functions and challenges with delivering proteins and peptides. These challenges include low permeability, enzyme degradation, short half-life, and immunogenicity. The document outlines various barriers to protein delivery, including enzymatic barriers and barriers at the intestinal epithelium, capillary endothelium, and blood-brain barrier. It also discusses physicochemical properties of proteins and peptides that impact delivery. Finally, it reviews various routes of delivery such as parenteral, pulmonary, and transdermal routes and technologies used for delivery like liposomes, hydrogels, emulsions, and pumps.
Mucoadhesive drug delivery system interact with the mucus layer covering the mucosal epithelial surface, & mucin molecules & increase the residence time of the dosage form at the site of the absorption.
Mucoadhesive drug delivery system is a part of controlled delivery system.
Since the early 1980,the concept of Mucoadhesion has gained considerable interest in pharmaceutical technology.
combine mucoadhesive with enzyme inhibitory & penetration enhancer properties & improve the patient complaince.
MDDS have been devloped for buccal ,nasal,rectal &vaginal routes for both systemic & local effects.
Hydrophilic high mol. wt. such as peptides that cannot be administered & poor absorption ,then MDDS is best choice.
Mucoadhesiveinner layers called mucosa inner epithelial cell lining is covered with viscoelasticfluid
Composed of water and mucin.
Thickness varies from 40 μm to 300 μm
General composition of mucus
Water…………………………………..95%
Glycoproteinsand lipids……………..0.5-5%
Mineral salts……………………………1%
Free proteins…………………………..0.5-1%
The mechanism responsible in the formation of mucoadhesive bond
Step 1 : Wetting and swelling of the polymer(contact stage)
Step 2 : Interpenetration between the polymer chains and the mucosal membrane
Step 3 : Formation of bonds between the entangled chains (both known as consolidation stage)
Electronic theory
Wetting theory
Adsorption theory
Diffusion theory
Fracture theory
Advantages over other controlled oral controlled release systems by virtue of prolongation of residence of drug in GIT.
Targeting & localization of the dosage form at a specific site
-Painless administration.
-Low enzymatic activity & avoid of first pass metabolism
If MDDS are adhere too tightlgy because it is undesirable to exert too much force to remove the formulation after use,otherwise the mucosa could be injured.
-Some patient suffers unpleasent feeling.
-Unfortunately ,the lack of standardized techniques often leads to unclear results.
-costly drug delivery system
Sustained and controlled release drug delivery systemParul Sharma
This document discusses sustained and controlled release drug delivery systems (SR and CRDDS). It defines SR and CRDDS and lists their advantages and disadvantages. It describes factors that influence the release rate from these systems, including physicochemical factors like solubility and biological factors like metabolism. The document outlines various physicochemical approaches to SR and CRDDS like matrix systems, reservoir systems, and ion exchange systems. It also discusses biological approaches using biopolymers and pulsatile release formulations. Finally, it briefly mentions applications and concludes with references.
DISSOLUTION
Dissolution is a process in which solid substance solubilizes in a given solvent
DISSOLUTION TESTING
A dissolution test uses an apparatus with specific test conditions in combination with acceptance criteria to evaluate the performance of the product. In-vitro test must predict the in-vivo behaviour
Factors in design of dissolution tests:
Factors relating to dissolution apparatus
Factors relation to dissolution fluid
Process parameters
Need of Dissolution Testing:
Development and optimisation of dosage forms
Batch to batch drug release uniformity
Quality, safety, efficacy and stability of the product
IVIV Correlation
Bioequivalence
Assessing pre and post approval changes
DISSOLUTION APPARATUS
Dissolution apparatus evolved to prepare a sample under controlled conditions thereby making the test repeatable.
Principle types of dissolution apparatus-
Close-compartment apparatus
Open-compartment apparatus
Dialysis systems
Ideal features of Dissolution Apparatus:
The fabrication, dimensions, and positioning of all components must be precisely specified and reproducible
Simple in design, easy to operate and useable
Sensitive
Nearly perfect sink conditions
Provide an easy means of introducing the dosage form into the dissolution medium
Provide minimum mechanical abrasion
Easy withdrawal of samples
Elimination of evaporation of solvent medium
DISSOLUTION METHODS
The Standard Dissolution Methods Database has been prepared by the Division of Bioequivalence, Office of Generic Drugs (OGD), Center for Drug Evaluation and Research (CDER), Food and Drug Administration (FDA).
Official methods:
Rotating Basket
Rotating Paddle
Reciprocating Cylinder
Flow-Through Cell
Paddle Over Disc
Rotating Cylinder
Reciprocating Disc
Non-official methods:
Static Disc Method
Beaker Method
Flask Stirrer Method
Peristalsis Method
Rotating Bottle Method
Dialysis Method
Diffusion Cell Method
Dissolution Apparatus Types and their Applications
Problems associated with dissolution apparatus
USP Performance Verification Test (PVT):
The USP Performance Verification Test (PVT) assesses the suitable performance of apparatus used in dissolution testing.
Responsible for detecting problems associated with the dissolution apparatus that are found to be within mechanical tolerances.
REFERENCES
This document discusses microspheres and microencapsulation. It was submitted by Debasish Deka for his M. Pharm degree under the guidance of Ananta Choudhury. It covers the introduction, advantages, limitations, types (e.g. bioadhesive, magnetic, floating), methods of preparation (e.g. solvent evaporation, spray drying), evaluation, and applications of microspheres in pharmaceutical industry (e.g. buccal drug delivery, intratumoral delivery). Microencapsulation is also introduced as enclosing solids, liquids or gases in microscopic particles through thin coatings, with origins in the 1930s business machines industry.
NIOSOMES , GENERAL CHARACTERISTICS OF NIOSOME , TYPES OF NIOSOMES , OTHERS TYPES OF NIOSOMES , NIOSOMES VS LIPOSOMES , COMPONENTS OF NIOSOMES , Non-ionic surfactant , Cholesterol , Charge inducing molecule , METHOD OF PREPARATION , preparation of small unilamellar vesicles , Sonication , Micro fluidization , preparation of large unilamellar vesicles , Reverse Phase Evaporation , Ether Injection , preparation of Multilamellar vesicles , Hand shaking method , Trans membrane pH gradient drug uptake process (remote loading) , Miscellaneous method :Multiple membrane extrusion method , The “Bubble” Method , Formation of Niosomes From Proniosomes , SEPARATION OF UNENTRAPPED DRUGS , Gel Filtration , Dialysis , Centrifugation , FACTORS AFFECTING THE PHYSICOCHEMICAL PROPERTIES OF NIOSOMES , Membrane Additives , Temperature of Hydration , PROPERTIES OF DRUGS , AMOUNT AND TYPE OF SURFACTANT
Structure of Surfactants , Resistance to Osmotic Stress , Characterization of niosomes ,Therapeutic applications of Niosomes , For Controlled Release of Drugs , To Improve the Stability and Physical Properties of the Drugs , For Targeting and Retention of Drug in Blood Circulation , Proniosomes , Aspasomes , Vesicles in Water and Oil System (v/w/o) ,Bola - niosomes , Discomes , Deformable niosomes or elastic niosomes , According to the nature of lamellarity ,Small Unilamellar vesicles (SUV) 25 – 500 nm in size.,Large Unilamellar vesicles (LUV) 0.1 – 1μm in size , Multilamellar vesicles (MLV) 1-5 μm in size , According to the size:Small Niosomes (100 nm – 200 nm) , Large Niosomes (800 nm – 900 nm),Big Niosomes (2 μm – 4 μm)
Mucoadhesive drug delivery system Mali vv pptVidhyaMali1
This document discusses mucoadhesive drug delivery systems (MDDS). It begins by defining MDDS as systems that use the bioadhesive properties of certain polymers to target and prolong the release of drugs at mucous membranes. It then covers the basics of mucous membranes and their structure, composition, and functions. The document discusses the need for MDDS to enhance drug absorption, prolong drug residence time, and target drug delivery. It also outlines the advantages and disadvantages of MDDS, various routes of administration, mechanisms of mucoadhesion, theories of mucoadhesion, mucoadhesive polymers, and methods of evaluating MDDS. In the end, it provides some applications of MDDS such as vaccine delivery, cancer
Zahid enzyme activated and osmotic pressure activated drug deliveryZahid1392
The document discusses different types of rate-controlled drug delivery systems (DDS), focusing on osmotic drug delivery systems and enzyme-activated drug delivery systems. It defines osmosis and osmotic pressure, and describes how osmotic DDS work using a semi-permeable membrane, drug reservoir, and osmotic agent to release drug at a controlled rate. It also outlines the basic components of osmotic DDS and how they are evaluated. Enzyme-activated DDS are described as relying on enzymatic hydrolysis of biopolymers like albumin by specific enzymes to activate drug release. Examples of marketed osmotic DDS products are provided.
This document provides an overview of pulmonary drug delivery systems. It discusses the anatomy and physiology of the lungs, advantages and disadvantages of pulmonary delivery, and different technologies used. Aerosols, propellants, and container types are described. Current pulmonary delivery devices discussed include metered dose inhalers, dry powder inhalers, and nebulizers. The document also covers evaluation methods for pharmaceutical aerosols and pulmonary drug delivery systems such as cascade impactors and in vitro and in vivo tests.
Description about a type of activation modulated drug delivery system, which a type of control drug delivery system.
Also, give a detailed description about each subclassification.
CrDDS is one which delivers the drug at a predetermined rate, for locally or systematically, for a prolong period of time.
Microencapsulation is a process where core materials are surrounded by a continuous film of polymeric material to form microparticles or microcapsules between 3-800μm in size. There are various techniques to microencapsulate such as spray drying, pan coating, and polymerization. Microencapsulation can increase bioavailability, alter drug release, and provide targeted drug delivery. Evaluation of the microcapsules involves measuring yield percentage, particle size, drug content, encapsulation efficiency, and in vitro drug release.
Gastro retentive drug delivery system (GRDDS)Ravish Yadav
gastro retentive drug delivery system topic include
1. introduction
2.advantages
3.technology
4.evaluation
5.disadvantages
6. matrix tablet
and other relative information regarding the topic
Polymers Used in Pharmaceutical SciencesOyshe Ahmed
INTRODUCTION
CLASSIFICATION AND CHARACTERISTICS OF POLYMERS
MECHANISM OF DRUG RELEASE FROM POLYMER
BIO DEGRADATION OF POLYMERS
SYNTHESIS OF POLYMERS
POLYMERS USED IN FORMULATION OF DIFFERENT DRUG DELIVERY SYSTEM.
APPLICATION OF POLYMERS
Sustained and Controlled Release (SR/CR)Prachi Pandey
This document discusses sustained release (SR) and controlled release (CR) drug delivery systems. SR systems provide medication over an extended period, usually 8-12 hours, following first-order kinetics. CR systems maintain constant drug levels by releasing the drug at a predetermined rate following zero-order kinetics. SR systems do not necessarily localize drug to the active site, while CR systems often do. SR and CR delivery can reduce side effects and dosing frequency while improving bioavailability and patient compliance compared to conventional dosage forms. Factors like dosage form materials, drug properties, and environment affect drug release from these systems.
This document discusses rate-controlled drug delivery systems. It defines sustained release and controlled release, with controlled release implying predictability and reproducibility in drug release kinetics. An ideal controlled delivery system delivers drugs at predetermined rates for specified times. Rate-preprogrammed systems release drugs at pre-set rates through polymer membranes, matrices, or microreservoirs. Activation-modulated systems activate drug release through physical, chemical, or biochemical processes. Examples of activation methods include osmotic pressure, hydrodynamic pressure, vapor pressure, and magnetism.
The document discusses microspheres as carriers for controlled drug delivery. It defines microspheres as small, insoluble, spherical particles consisting of a polymer matrix and drug. Various methods for preparing microspheres are described, including single and double emulsion techniques. Characterization techniques like particle size analysis and release studies are also summarized. Potential applications of microspheres include vaccine delivery, targeted drug delivery to specific sites like the eyes, and controlled release formulations.
This document provides an overview of microspheres, including their definition, classification, preparation methods, characterization, applications, and examples of marketed microsphere products. Microspheres are small spherical particles made of polymers, lipids, or waxes that are used for drug delivery applications to provide controlled or sustained release of pharmaceutical actives. Common preparation methods include single and double emulsion techniques, phase separation processes, and spray drying. Microspheres are characterized based on properties like particle size, shape, drug loading, and in vitro drug release. They have applications in areas like vaccine delivery, cancer treatment, and oral drug delivery for prolonged release. Examples of commercial microsphere products mentioned include Expancel microspheres and BioMag Protein A particles.
This document discusses microcapsules and microspheres, including their types, sizes, materials used, and preparation methods. Microcapsules contain an active agent surrounded by a polymeric shell, while microspheres are small spherical particles made of polymers, glass, or ceramics between 1-1000 microns in diameter. Common preparation methods include emulsion polymerization, interfacial polycondensation, suspension crosslinking, solvent evaporation/extraction, and coacervation/phase separation.
Microspheres and microcapsules are spherical particles ranging from 1 μm to 1000 μm in diameter that can be used to encapsulate drugs for controlled release. Microspheres contain drug distributed throughout while microcapsules contain drug enclosed within a coating. Various natural and synthetic polymers are used to prepare microspheres and microcapsules through techniques like solvent evaporation, emulsion polymerization, and coacervation. Microspheres and microcapsules offer benefits like sustained drug release, targeted drug delivery, and reduced dosing frequency. They are evaluated based on particle size, drug entrapment efficiency, in vitro drug release, and other physicochemical properties.
This document discusses various analytical techniques used to evaluate protein and peptide drug formulations, including stability testing, bioassays, UV spectroscopy, Bradford assay, differential scanning calorimetry, chromatography, and electrophoresis. Stability testing evaluates how environmental factors affect the quality of a drug over time. Bioassays assess potency by monitoring the in vitro or in vivo pharmacological response to the protein. UV spectroscopy, Bradford assay, and electrophoresis can be used to detect and quantify the amount of protein present in a sample. Chromatography and differential scanning calorimetry provide information about stability and conformational changes of proteins.
Protein and-peptide-drug-delivery-systemsGaurav Kr
The document discusses protein and peptide drug delivery systems. It begins by defining proteins and peptides, noting that proteins are molecules composed of over 50 amino acids, while peptides are molecules composed of less than 50 amino acids. It then discusses how scientific advances in molecular and cell biology have led to the development of recombinant DNA and hybridoma technology to produce protein products. The document provides examples of marketed protein and peptide drugs and discusses challenges with delivering these drugs orally due to their large molecular size and susceptibility to enzymatic degradation. It explores approaches to protein and peptide delivery including non-parenteral systemic delivery methods and various considerations for developing delivery systems for these pharmaceuticals.
Content:
Introduction
Ideal Properties
Advantages
Limitations
Types of Microsphere
Method for Preparation
Polymer Used for Preparation
Release of Drug from Microsphere
Application
This document provides an overview of protein and peptide drug delivery. It begins with definitions of proteins and peptides and descriptions of protein structure. It then discusses protein functions and challenges with delivering proteins and peptides. These challenges include low permeability, enzyme degradation, short half-life, and immunogenicity. The document outlines various barriers to protein delivery, including enzymatic barriers and barriers at the intestinal epithelium, capillary endothelium, and blood-brain barrier. It also discusses physicochemical properties of proteins and peptides that impact delivery. Finally, it reviews various routes of delivery such as parenteral, pulmonary, and transdermal routes and technologies used for delivery like liposomes, hydrogels, emulsions, and pumps.
Mucoadhesive drug delivery system interact with the mucus layer covering the mucosal epithelial surface, & mucin molecules & increase the residence time of the dosage form at the site of the absorption.
Mucoadhesive drug delivery system is a part of controlled delivery system.
Since the early 1980,the concept of Mucoadhesion has gained considerable interest in pharmaceutical technology.
combine mucoadhesive with enzyme inhibitory & penetration enhancer properties & improve the patient complaince.
MDDS have been devloped for buccal ,nasal,rectal &vaginal routes for both systemic & local effects.
Hydrophilic high mol. wt. such as peptides that cannot be administered & poor absorption ,then MDDS is best choice.
Mucoadhesiveinner layers called mucosa inner epithelial cell lining is covered with viscoelasticfluid
Composed of water and mucin.
Thickness varies from 40 μm to 300 μm
General composition of mucus
Water…………………………………..95%
Glycoproteinsand lipids……………..0.5-5%
Mineral salts……………………………1%
Free proteins…………………………..0.5-1%
The mechanism responsible in the formation of mucoadhesive bond
Step 1 : Wetting and swelling of the polymer(contact stage)
Step 2 : Interpenetration between the polymer chains and the mucosal membrane
Step 3 : Formation of bonds between the entangled chains (both known as consolidation stage)
Electronic theory
Wetting theory
Adsorption theory
Diffusion theory
Fracture theory
Advantages over other controlled oral controlled release systems by virtue of prolongation of residence of drug in GIT.
Targeting & localization of the dosage form at a specific site
-Painless administration.
-Low enzymatic activity & avoid of first pass metabolism
If MDDS are adhere too tightlgy because it is undesirable to exert too much force to remove the formulation after use,otherwise the mucosa could be injured.
-Some patient suffers unpleasent feeling.
-Unfortunately ,the lack of standardized techniques often leads to unclear results.
-costly drug delivery system
Sustained and controlled release drug delivery systemParul Sharma
This document discusses sustained and controlled release drug delivery systems (SR and CRDDS). It defines SR and CRDDS and lists their advantages and disadvantages. It describes factors that influence the release rate from these systems, including physicochemical factors like solubility and biological factors like metabolism. The document outlines various physicochemical approaches to SR and CRDDS like matrix systems, reservoir systems, and ion exchange systems. It also discusses biological approaches using biopolymers and pulsatile release formulations. Finally, it briefly mentions applications and concludes with references.
DISSOLUTION
Dissolution is a process in which solid substance solubilizes in a given solvent
DISSOLUTION TESTING
A dissolution test uses an apparatus with specific test conditions in combination with acceptance criteria to evaluate the performance of the product. In-vitro test must predict the in-vivo behaviour
Factors in design of dissolution tests:
Factors relating to dissolution apparatus
Factors relation to dissolution fluid
Process parameters
Need of Dissolution Testing:
Development and optimisation of dosage forms
Batch to batch drug release uniformity
Quality, safety, efficacy and stability of the product
IVIV Correlation
Bioequivalence
Assessing pre and post approval changes
DISSOLUTION APPARATUS
Dissolution apparatus evolved to prepare a sample under controlled conditions thereby making the test repeatable.
Principle types of dissolution apparatus-
Close-compartment apparatus
Open-compartment apparatus
Dialysis systems
Ideal features of Dissolution Apparatus:
The fabrication, dimensions, and positioning of all components must be precisely specified and reproducible
Simple in design, easy to operate and useable
Sensitive
Nearly perfect sink conditions
Provide an easy means of introducing the dosage form into the dissolution medium
Provide minimum mechanical abrasion
Easy withdrawal of samples
Elimination of evaporation of solvent medium
DISSOLUTION METHODS
The Standard Dissolution Methods Database has been prepared by the Division of Bioequivalence, Office of Generic Drugs (OGD), Center for Drug Evaluation and Research (CDER), Food and Drug Administration (FDA).
Official methods:
Rotating Basket
Rotating Paddle
Reciprocating Cylinder
Flow-Through Cell
Paddle Over Disc
Rotating Cylinder
Reciprocating Disc
Non-official methods:
Static Disc Method
Beaker Method
Flask Stirrer Method
Peristalsis Method
Rotating Bottle Method
Dialysis Method
Diffusion Cell Method
Dissolution Apparatus Types and their Applications
Problems associated with dissolution apparatus
USP Performance Verification Test (PVT):
The USP Performance Verification Test (PVT) assesses the suitable performance of apparatus used in dissolution testing.
Responsible for detecting problems associated with the dissolution apparatus that are found to be within mechanical tolerances.
REFERENCES
This document discusses microspheres and microencapsulation. It was submitted by Debasish Deka for his M. Pharm degree under the guidance of Ananta Choudhury. It covers the introduction, advantages, limitations, types (e.g. bioadhesive, magnetic, floating), methods of preparation (e.g. solvent evaporation, spray drying), evaluation, and applications of microspheres in pharmaceutical industry (e.g. buccal drug delivery, intratumoral delivery). Microencapsulation is also introduced as enclosing solids, liquids or gases in microscopic particles through thin coatings, with origins in the 1930s business machines industry.
NIOSOMES , GENERAL CHARACTERISTICS OF NIOSOME , TYPES OF NIOSOMES , OTHERS TYPES OF NIOSOMES , NIOSOMES VS LIPOSOMES , COMPONENTS OF NIOSOMES , Non-ionic surfactant , Cholesterol , Charge inducing molecule , METHOD OF PREPARATION , preparation of small unilamellar vesicles , Sonication , Micro fluidization , preparation of large unilamellar vesicles , Reverse Phase Evaporation , Ether Injection , preparation of Multilamellar vesicles , Hand shaking method , Trans membrane pH gradient drug uptake process (remote loading) , Miscellaneous method :Multiple membrane extrusion method , The “Bubble” Method , Formation of Niosomes From Proniosomes , SEPARATION OF UNENTRAPPED DRUGS , Gel Filtration , Dialysis , Centrifugation , FACTORS AFFECTING THE PHYSICOCHEMICAL PROPERTIES OF NIOSOMES , Membrane Additives , Temperature of Hydration , PROPERTIES OF DRUGS , AMOUNT AND TYPE OF SURFACTANT
Structure of Surfactants , Resistance to Osmotic Stress , Characterization of niosomes ,Therapeutic applications of Niosomes , For Controlled Release of Drugs , To Improve the Stability and Physical Properties of the Drugs , For Targeting and Retention of Drug in Blood Circulation , Proniosomes , Aspasomes , Vesicles in Water and Oil System (v/w/o) ,Bola - niosomes , Discomes , Deformable niosomes or elastic niosomes , According to the nature of lamellarity ,Small Unilamellar vesicles (SUV) 25 – 500 nm in size.,Large Unilamellar vesicles (LUV) 0.1 – 1μm in size , Multilamellar vesicles (MLV) 1-5 μm in size , According to the size:Small Niosomes (100 nm – 200 nm) , Large Niosomes (800 nm – 900 nm),Big Niosomes (2 μm – 4 μm)
Mucoadhesive drug delivery system Mali vv pptVidhyaMali1
This document discusses mucoadhesive drug delivery systems (MDDS). It begins by defining MDDS as systems that use the bioadhesive properties of certain polymers to target and prolong the release of drugs at mucous membranes. It then covers the basics of mucous membranes and their structure, composition, and functions. The document discusses the need for MDDS to enhance drug absorption, prolong drug residence time, and target drug delivery. It also outlines the advantages and disadvantages of MDDS, various routes of administration, mechanisms of mucoadhesion, theories of mucoadhesion, mucoadhesive polymers, and methods of evaluating MDDS. In the end, it provides some applications of MDDS such as vaccine delivery, cancer
Zahid enzyme activated and osmotic pressure activated drug deliveryZahid1392
The document discusses different types of rate-controlled drug delivery systems (DDS), focusing on osmotic drug delivery systems and enzyme-activated drug delivery systems. It defines osmosis and osmotic pressure, and describes how osmotic DDS work using a semi-permeable membrane, drug reservoir, and osmotic agent to release drug at a controlled rate. It also outlines the basic components of osmotic DDS and how they are evaluated. Enzyme-activated DDS are described as relying on enzymatic hydrolysis of biopolymers like albumin by specific enzymes to activate drug release. Examples of marketed osmotic DDS products are provided.
This document provides an overview of pulmonary drug delivery systems. It discusses the anatomy and physiology of the lungs, advantages and disadvantages of pulmonary delivery, and different technologies used. Aerosols, propellants, and container types are described. Current pulmonary delivery devices discussed include metered dose inhalers, dry powder inhalers, and nebulizers. The document also covers evaluation methods for pharmaceutical aerosols and pulmonary drug delivery systems such as cascade impactors and in vitro and in vivo tests.
Description about a type of activation modulated drug delivery system, which a type of control drug delivery system.
Also, give a detailed description about each subclassification.
CrDDS is one which delivers the drug at a predetermined rate, for locally or systematically, for a prolong period of time.
Microencapsulation is a process where core materials are surrounded by a continuous film of polymeric material to form microparticles or microcapsules between 3-800μm in size. There are various techniques to microencapsulate such as spray drying, pan coating, and polymerization. Microencapsulation can increase bioavailability, alter drug release, and provide targeted drug delivery. Evaluation of the microcapsules involves measuring yield percentage, particle size, drug content, encapsulation efficiency, and in vitro drug release.
Gastro retentive drug delivery system (GRDDS)Ravish Yadav
gastro retentive drug delivery system topic include
1. introduction
2.advantages
3.technology
4.evaluation
5.disadvantages
6. matrix tablet
and other relative information regarding the topic
Polymers Used in Pharmaceutical SciencesOyshe Ahmed
INTRODUCTION
CLASSIFICATION AND CHARACTERISTICS OF POLYMERS
MECHANISM OF DRUG RELEASE FROM POLYMER
BIO DEGRADATION OF POLYMERS
SYNTHESIS OF POLYMERS
POLYMERS USED IN FORMULATION OF DIFFERENT DRUG DELIVERY SYSTEM.
APPLICATION OF POLYMERS
Sustained and Controlled Release (SR/CR)Prachi Pandey
This document discusses sustained release (SR) and controlled release (CR) drug delivery systems. SR systems provide medication over an extended period, usually 8-12 hours, following first-order kinetics. CR systems maintain constant drug levels by releasing the drug at a predetermined rate following zero-order kinetics. SR systems do not necessarily localize drug to the active site, while CR systems often do. SR and CR delivery can reduce side effects and dosing frequency while improving bioavailability and patient compliance compared to conventional dosage forms. Factors like dosage form materials, drug properties, and environment affect drug release from these systems.
This document discusses rate-controlled drug delivery systems. It defines sustained release and controlled release, with controlled release implying predictability and reproducibility in drug release kinetics. An ideal controlled delivery system delivers drugs at predetermined rates for specified times. Rate-preprogrammed systems release drugs at pre-set rates through polymer membranes, matrices, or microreservoirs. Activation-modulated systems activate drug release through physical, chemical, or biochemical processes. Examples of activation methods include osmotic pressure, hydrodynamic pressure, vapor pressure, and magnetism.
The document discusses microspheres as carriers for controlled drug delivery. It defines microspheres as small, insoluble, spherical particles consisting of a polymer matrix and drug. Various methods for preparing microspheres are described, including single and double emulsion techniques. Characterization techniques like particle size analysis and release studies are also summarized. Potential applications of microspheres include vaccine delivery, targeted drug delivery to specific sites like the eyes, and controlled release formulations.
This document provides an overview of microspheres, including their definition, classification, preparation methods, characterization, applications, and examples of marketed microsphere products. Microspheres are small spherical particles made of polymers, lipids, or waxes that are used for drug delivery applications to provide controlled or sustained release of pharmaceutical actives. Common preparation methods include single and double emulsion techniques, phase separation processes, and spray drying. Microspheres are characterized based on properties like particle size, shape, drug loading, and in vitro drug release. They have applications in areas like vaccine delivery, cancer treatment, and oral drug delivery for prolonged release. Examples of commercial microsphere products mentioned include Expancel microspheres and BioMag Protein A particles.
In this ppt ,i have covered the introduction of microspheres,various preparation methods of microspheres, advantages and disadvantage of microspheres,types and evaluation parameters of the microspheres.
Introduction
Need of Nanosuspension
Advantages of Nanosuspension
Disadvantages of Nanosuspension
Method Of Preparation
Formulation Considerations
Characterization of Nanosuspension
Current Marketed Formulations
Pharmaceutical Applications
Liposomes are spherical vesicles made of phospholipid bilayers that can encapsulate hydrophilic or hydrophobic drugs. They offer several advantages for drug delivery such as protection of encapsulated drugs, controlled release, targeted delivery, and improved pharmacokinetics. There are various methods for preparing liposomes of different sizes and compositions, with the most common being lipid hydration, sonication, and extrusion. Liposomes must be characterized based on their size, lamellarity, drug encapsulation efficiency, and stability to ensure quality for pharmaceutical applications such as drug delivery.
Microspheres by Neelam somani and Meenakshi BharkatiyaNEELAMSOMANI4
Microspheres are small spherical particles between 1μm to 1000μm in diameter that can be made from proteins or synthetic polymers. They are used for drug delivery and can be classified as microcapsules, which contain an entrapped substance surrounded by a capsule wall, or micromatrices, where the substance is dispersed throughout the matrix. Common types include bioadhesive, floating, radioactive, magnetic, and polymeric microspheres. Microspheres offer benefits like improved drug bioavailability, constant therapeutic effects, and protection of drugs from degradation. They are prepared using techniques like single or double emulsion, polymerization, coacervation, spray drying, and solvent extraction.
A note on Microsperes , general introduction and method of preparationsNEELAMSOMANI4
This presentation is related to Microspheres. Microspheres as a part of novel drug delivery system relevant to Pharmaceutics. The general introductions and methodology is described that will be helpful to all pharmacy students .
This document summarizes a seminar presentation on microemulsions given by Mr. Vishal R. Mohite under the guidance of Prof. K. K. Mali. It introduces emulsions and the differences between emulsions and microemulsions. The advantages and types of microemulsions are discussed. The key components, structure, preparation methods, and applications of microemulsions in drug delivery are described, including uses for oral, parenteral, topical, ophthalmic, nasal, and periodontal delivery.
Microsponges are polymeric delivery systems composed of porous microspheres that can be used to deliver drugs topically, orally, and for biomedical applications. They provide controlled release of active ingredients, increase drug payload, and reduce side effects. The document discusses the preparation, characterization, and various applications of microsponge drug delivery systems.
New microsoft office power point presentationMayuri Yadav
This document provides an introduction and overview of nanosuspensions for pharmaceutical applications. It was prepared by Mayuri B. Yadav and guided by Prof. Dr. S. N. Dhole of Modern College of Pharmacy in Pune, India. The document defines nanosuspensions and discusses their advantages such as improved bioavailability. It also outlines various preparation methods including media milling, high pressure homogenization, and the use of emulsions or microemulsions as templates. Evaluation parameters for nanosuspensions and some currently marketed formulations are also mentioned. The applications and conclusion state that nanosuspensions can effectively deliver poorly soluble drugs.
This document discusses self-emulsified drug delivery systems (SEDDS), which are isotropic mixtures of drugs, lipids, and surfactants that can spontaneously form emulsions upon dilution in aqueous media. SEDDS aim to improve oral absorption of hydrophobic drugs. The document covers classification systems for lipid formulations, formulation development techniques like screening excipients and conducting studies, characterization methods, and solid forms of SEDDS like capsules. It also discusses biopharmaceutical issues like the role of lipolysis and drug transport via the lymphatic system. Several commercial products incorporating SEDDS are also mentioned.
Microspheres are small spherical particles typically between 1-1000 micrometers in diameter. They are made of natural or synthetic polymers and can be used for sustained drug delivery. Microspheres encapsulate drugs either molecularly or in particle form throughout a polymer matrix. They offer benefits like prolonged release, reduced dosing, and ability to inject. Microspheres can be made using various techniques like single/double emulsion, solvent evaporation, phase separation. Characterization methods include particle size analysis, drug entrapment efficiency, in vitro drug release, and stability studies. Microspheres show potential for targeted and controlled drug delivery.
This document discusses ocular drug delivery systems. It begins by outlining the ideal characteristics of an ophthalmic delivery system. It then describes various advanced, controlled, particulate, and vesicular drug delivery systems for ocular administration. It discusses limitations of conventional eye drops and advantages of advanced delivery systems. Factors affecting intraocular bioavailability are highlighted. The objectives and approaches to improve ocular drug delivery, including enhancement of bioavailability and various dosage forms are summarized.
FORMULATION AND EVALUATION OF GLIBENCLAMIDE MICROSPHERE DRUG DELIVERY SYSTEMArindam Chakraborty
The document discusses the formulation and evaluation of glibenclamide microsphere drug delivery system. The objective was to increase the drug's self-life by developing a microsphere delivery system. Two batches of glibenclamide microspheres were prepared using different polymers and manufacturing methods. Batch 2, prepared via spray congealing with agar polymer, showed more sustained release over 12 hours compared to Batch 1 and was considered the optimized formulation. In vitro drug release studies found Batch 2 followed zero-order kinetics. The microspheres were characterized and evaluated for properties like particle size, drug entrapment efficiency, and in vitro drug release kinetics. The study achieved sustained drug release to improve bioavailability and patient compliance.
Rahul Molla's document discusses recent advances in nanosponges as a drug delivery system. Nanosponges are porous polymeric particles that can be used for controlled drug delivery through various routes of administration including topical, oral, and parenteral. The document outlines the advantages of nanosponges such as increased drug solubility and controlled release as well as factors that influence nanosponge formulation and common preparation methods. Evaluation techniques for nanosponges including particle size, drug loading efficiency, and in vitro drug release are also summarized. Finally, the document discusses applications of nanosponges in cancer therapy, topical drug delivery, and antiviral delivery.
Microencapsulation involves coating tiny liquid or solid particles with a polymeric film. It has advantages like increasing bioavailability, altering drug release, and improving compliance. Common techniques include coacervation, solvent evaporation, spray drying, and polymerization. Microencapsulation can protect ingredients, mask tastes, and provide targeted delivery for applications like food, pharma, and agriculture.
Microspheres are solid spherical particles ranging from 1-1000μm that are used for drug delivery. They can be made of proteins or synthetic polymers. There are two main types - microcapsules which have a core and coating, and micromatrices which have a drug dispersed throughout the polymer matrix. Microspheres offer advantages like reduced dosing, constant drug levels, and protection of drugs. They are made using methods like solvent evaporation, emulsion techniques, and polymerization. Microspheres find applications in delivery to sites like the eyes, oral cavity, skin and more. Evaluation involves analyzing size, shape, drug content and release kinetics.
This document discusses microspheres and magnetic microspheres. It defines magnetic microspheres as microspheres containing magnetic substances that can be targeted using an external magnetic field. The document covers concepts like using magnetic microspheres for targeted drug delivery and their advantages like preventing rapid clearance and achieving controlled drug release. Preparation methods like single and double emulsion techniques are summarized. Characterization techniques and applications in areas like vaccine delivery and imaging are also mentioned.
Liposomes are artificially created spherical vesicles made of phospholipids and cholesterol that can encapsulate both hydrophilic and hydrophobic drugs. They are promising drug delivery systems due to their biocompatibility and ability to selectively target tissues. Liposomes vary in size from 20-5000 nm and consist of one or more phospholipid bilayers surrounding an aqueous core. There are several methods for preparing and loading drugs into liposomes to develop drug delivery systems with benefits like increased drug efficacy, stability and reduced toxicity.
Similar to microsphere as drug delivery system (20)
These lecture slides, by Dr Sidra Arshad, offer a quick overview of the physiological basis of a normal electrocardiogram.
Learning objectives:
1. Define an electrocardiogram (ECG) and electrocardiography
2. Describe how dipoles generated by the heart produce the waveforms of the ECG
3. Describe the components of a normal electrocardiogram of a typical bipolar lead (limb II)
4. Differentiate between intervals and segments
5. Enlist some common indications for obtaining an ECG
6. Describe the flow of current around the heart during the cardiac cycle
7. Discuss the placement and polarity of the leads of electrocardiograph
8. Describe the normal electrocardiograms recorded from the limb leads and explain the physiological basis of the different records that are obtained
9. Define mean electrical vector (axis) of the heart and give the normal range
10. Define the mean QRS vector
11. Describe the axes of leads (hexagonal reference system)
12. Comprehend the vectorial analysis of the normal ECG
13. Determine the mean electrical axis of the ventricular QRS and appreciate the mean axis deviation
14. Explain the concepts of current of injury, J point, and their significance
Study Resources:
1. Chapter 11, Guyton and Hall Textbook of Medical Physiology, 14th edition
2. Chapter 9, Human Physiology - From Cells to Systems, Lauralee Sherwood, 9th edition
3. Chapter 29, Ganong’s Review of Medical Physiology, 26th edition
4. Electrocardiogram, StatPearls - https://www.ncbi.nlm.nih.gov/books/NBK549803/
5. ECG in Medical Practice by ABM Abdullah, 4th edition
6. Chapter 3, Cardiology Explained, https://www.ncbi.nlm.nih.gov/books/NBK2214/
7. ECG Basics, http://www.nataliescasebook.com/tag/e-c-g-basics
Muktapishti is a traditional Ayurvedic preparation made from Shoditha Mukta (Purified Pearl), is believed to help regulate thyroid function and reduce symptoms of hyperthyroidism due to its cooling and balancing properties. Clinical evidence on its efficacy remains limited, necessitating further research to validate its therapeutic benefits.
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Does Over-Masturbation Contribute to Chronic Prostatitis.pptxwalterHu5
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Travel vaccination in Manchester offers comprehensive immunization services for individuals planning international trips. Expert healthcare providers administer vaccines tailored to your destination, ensuring you stay protected against various diseases. Conveniently located clinics and flexible appointment options make it easy to get the necessary shots before your journey. Stay healthy and travel with confidence by getting vaccinated in Manchester. Visit us: www.nxhealthcare.co.uk
Cell Therapy Expansion and Challenges in Autoimmune DiseaseHealth Advances
There is increasing confidence that cell therapies will soon play a role in the treatment of autoimmune disorders, but the extent of this impact remains to be seen. Early readouts on autologous CAR-Ts in lupus are encouraging, but manufacturing and cost limitations are likely to restrict access to highly refractory patients. Allogeneic CAR-Ts have the potential to broaden access to earlier lines of treatment due to their inherent cost benefits, however they will need to demonstrate comparable or improved efficacy to established modalities.
In addition to infrastructure and capacity constraints, CAR-Ts face a very different risk-benefit dynamic in autoimmune compared to oncology, highlighting the need for tolerable therapies with low adverse event risk. CAR-NK and Treg-based therapies are also being developed in certain autoimmune disorders and may demonstrate favorable safety profiles. Several novel non-cell therapies such as bispecific antibodies, nanobodies, and RNAi drugs, may also offer future alternative competitive solutions with variable value propositions.
Widespread adoption of cell therapies will not only require strong efficacy and safety data, but also adapted pricing and access strategies. At oncology-based price points, CAR-Ts are unlikely to achieve broad market access in autoimmune disorders, with eligible patient populations that are potentially orders of magnitude greater than the number of currently addressable cancer patients. Developers have made strides towards reducing cell therapy COGS while improving manufacturing efficiency, but payors will inevitably restrict access until more sustainable pricing is achieved.
Despite these headwinds, industry leaders and investors remain confident that cell therapies are poised to address significant unmet need in patients suffering from autoimmune disorders. However, the extent of this impact on the treatment landscape remains to be seen, as the industry rapidly approaches an inflection point.
Adhd Medication Shortage Uk - trinexpharmacy.comreignlana06
The UK is currently facing a Adhd Medication Shortage Uk, which has left many patients and their families grappling with uncertainty and frustration. ADHD, or Attention Deficit Hyperactivity Disorder, is a chronic condition that requires consistent medication to manage effectively. This shortage has highlighted the critical role these medications play in the daily lives of those affected by ADHD. Contact : +1 (747) 209 – 3649 E-mail : sales@trinexpharmacy.com
share - Lions, tigers, AI and health misinformation, oh my!.pptxTina Purnat
• Pitfalls and pivots needed to use AI effectively in public health
• Evidence-based strategies to address health misinformation effectively
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Local Advanced Lung Cancer: Artificial Intelligence, Synergetics, Complex Sys...Oleg Kshivets
Overall life span (LS) was 1671.7±1721.6 days and cumulative 5YS reached 62.4%, 10 years – 50.4%, 20 years – 44.6%. 94 LCP lived more than 5 years without cancer (LS=2958.6±1723.6 days), 22 – more than 10 years (LS=5571±1841.8 days). 67 LCP died because of LC (LS=471.9±344 days). AT significantly improved 5YS (68% vs. 53.7%) (P=0.028 by log-rank test). Cox modeling displayed that 5YS of LCP significantly depended on: N0-N12, T3-4, blood cell circuit, cell ratio factors (ratio between cancer cells-CC and blood cells subpopulations), LC cell dynamics, recalcification time, heparin tolerance, prothrombin index, protein, AT, procedure type (P=0.000-0.031). Neural networks, genetic algorithm selection and bootstrap simulation revealed relationships between 5YS and N0-12 (rank=1), thrombocytes/CC (rank=2), segmented neutrophils/CC (3), eosinophils/CC (4), erythrocytes/CC (5), healthy cells/CC (6), lymphocytes/CC (7), stick neutrophils/CC (8), leucocytes/CC (9), monocytes/CC (10). Correct prediction of 5YS was 100% by neural networks computing (error=0.000; area under ROC curve=1.0).
Local Advanced Lung Cancer: Artificial Intelligence, Synergetics, Complex Sys...
microsphere as drug delivery system
1. 20SSRMPH06 SSR COLLEGE OF PHARMACY,SILVASSA JIDNESH DHARMAMEHER
SEMINAR ON :
“SALIENT PRESPECTIVES OF MICROSPHERE AS
A NOVEL DRUG DELIVERY SYSTEM”
2. 20SSRMPH06 SSR COLLEGE OF PHARMACY,SILVASSA JIDNESH DHARMAMEHER
PRESENTATION OUTLINE
INTRODUCTION
NEEDS OF MICROSPHERES
IDEAL CHARACTERISTICS
ADVANTAGES AND DISADVANTAGES
TYPES OF MICROSPHERES
MATERIAL USED IN PREPARATION
METHODS OF PREPARATION
EVALUATION
APPLICATION AND MARKETED FORMULATION
3. 20SSRMPH06 SSR COLLEGE OF PHARMACY,SILVASSA JIDNESH DHARMAMEHER
INTRODUCTION
Microspheres are multiparticulate drug delivery systems which
are prepared to obtain prolonged or controlled drug delivery to
improve bioavailability, stability and to target the drug to specific
site at a predetermined rate.
Microspheres are small spherical particles, with diameters 1 μm
to 1000 μm. They are spherical free flowing particles consisting
of proteins or synthetic polymers which are biodegradable in
nature.
Microspheres can be manufactured from various natural and
synthetic materials. Microsphere play an important role to
improve bioavailability of conventional drugs and minimizing
side effects.
4. 20SSRMPH06 SSR COLLEGE OF PHARMACY,SILVASSA JIDNESH DHARMAMEHER
Contd…
• There are three types of micropaerticulates:
MICROPARTICULATES
MICROCAPSULES
MICROMATRICES
polynuclear
5. 20SSRMPH06 SSR COLLEGE OF PHARMACY,SILVASSA JIDNESH DHARMAMEHER
NEEDS OF MICROSPHERES
Targeting of active drug moieties to specific body sites with
controlled and predetermined drug release from the drug delivery
systems have great impact on human health care.
Novel drug delivery technology provides an effective approach for
entrapment of therapeutically active drugs in multiple unit dosage
forms such as microparticles and nanoparticles etc, which transforms
the absorption and kinetic properties of the drug molecules.
Among multiple unit dosage forms microspheres plays an important
role in arena of particulate type of drug delivery systems due to
better entrapment, small size with good release characteristics.
These systems are coupled with various advantages such as
improved therapeutic efficacy with better compliance, encapsulation
of variety of drug molecules (macro and micromolecules) low toxicity
in comparison to conventional dosage forms.
Microspheres an innovative approach in drug delivery system,solanki
6. 20SSRMPH06 SSR COLLEGE OF PHARMACY,SILVASSA JIDNESH DHARMAMEHER
IDEAL CHARACTERISTICS
The ability to incorporate reasonably high concentrations of the drug.
Stability of the preparation after synthesis with a clinically acceptable
shelf life.
Controlled particle size and dispersability in aqueous vehicles for
injection.
Release of active reagent with a good control over a wide time scale.
Biocompatibility with a controllable biodegradability.
Susceptibility to chemical modification.
7. 20SSRMPH06 SSR COLLEGE OF PHARMACY,SILVASSA JIDNESH DHARMAMEHER
ADVANTAGES
These systems provide prolonged and constant therapeutic effect.
Reduces the dosing frequency and therefore improvement in patient compliance.
Microspheres produce more reproducible drug absorption.
Drug discharge in stomach is hindered and that’s why local unwanted effects are reduced.
In case of microspheres, better therapeutic effect for short half-life of drugs can be achieved.
Dose dumping effect can be reduced by microspheres.
Microspheres also reduce the chances of G.I. irritation.
Microspheres provide freedom from drug and recipients incompatibilities especially with
buffer.
Better protection of drugs against environment conditions.
Taste and odour of unpleasant drugs can be effectively masked.
Microspheres reduce the first pass metabolism.
Microspheres can be easily injected in body because of their small and spherical size.
Microspheres enhance the biological half-life and also improve the bioavailability.
8. 20SSRMPH06 SSR COLLEGE OF PHARMACY,SILVASSA JIDNESH DHARMAMEHER
DISADVANTAGES
The costs of the materials and processing of the controlled release
preparation, are substantially higher than those of standard
formulations.
The fate of polymer matrix and its effect on the environment.
The fate of polymer additives such as plasticizers, stabilizers,
antioxidants and fillers.
Reproducibility is less.
Process conditions like change in temperature, pH, solvent addition,
and evaporation/agitation may influence the stability of core particles
to be encapsulated.
The environmental impact of the degradation products of the
polymer matrix produced in response to heat, hydrolysis, oxidation,
solar radiation or biological agents.
9. 20SSRMPH06 SSR COLLEGE OF PHARMACY,SILVASSA JIDNESH DHARMAMEHER
METHODS OF PREPARATION
• Solvent evaporation
• Hot melt microencapsulation
• Solvent extraction
• Hydrogel microspheres
• Spray drying
• Phase inversion
• Alkaline co-precipitation
• Inverse phase sepration polymerization
• Sono chemical
• Spray cooling/chilling
• Pan coating
J.K. Vasir et al.
10. 20SSRMPH06 SSR COLLEGE OF PHARMACY,SILVASSA JIDNESH DHARMAMEHER
METHODS OF PREPARATION
• Solvent evaporation:
It is the most extensively used method of microencapsulation, first
described by Ogawa et al. (1988).
A buffered or plain aqueous solution of the drug (may contain a
viscosity building or stabilising agent) is added to an organic phase
consisting of the polymer solution in solvents like dichloromethane
(or ethyl acetate or chloroform) with vigorous stirring to form the
primary water in oil emulsion.
This emulsion is then added to a large volume of water containing an
emulsifier like PVA or PVP to form the multiple emulsion (w/o/w).
The double emulsion, so formed, is then subjected to stirring until
most of the organic solvent evaporates, leaving solid microspheres.
The microspheres can then be washed, centrifuged and lyophilised to
obtain the free flowing and dried microspheres.
11. 20SSRMPH06 SSR COLLEGE OF PHARMACY,SILVASSA JIDNESH DHARMAMEHER
METHODS OF PREPARATION
• Solvent evaporation:
12. 20SSRMPH06 SSR COLLEGE OF PHARMACY,SILVASSA JIDNESH DHARMAMEHER
METHODS OF PREPARATION
Hot melt microencapsulation:
This method was first used by Mathiowitz and Langer (1987) to
prepare microspheres of polyanhydride copolymer of poly[bis(p-
carboxy phenoxy) propane anhydride] with sebacic acid.
In this method, the polymer is first melted and then mixed with solid
particles of the drug that have been sieved to less than 50µm.
The mixture is suspended in a non-miscible solvent (like silicone oil),
continuously stirred, and heated to 5◦C above the melting point of
the polymer. Once the emulsion is stabilised, it is cooled until the
polymer particles solidify.
The resulting microspheres are washed by decantation with
petroleum ether.
13. 20SSRMPH06 SSR COLLEGE OF PHARMACY,SILVASSA JIDNESH DHARMAMEHER
METHODS OF PREPARATION
Hot melt microencapsulation:
The primary objective for developing this method is to develop a
microencapsulation process suitable for the water labile
polymers, e.g. polyanhydrides.
Microspheres with diameter of 1–1000 µm can be obtained and
the size distribution can be easily controlled by altering the
stirring rate.
The only disadvantage of this method is the moderate
temperature towhich drug is exposed.
14. 20SSRMPH06 SSR COLLEGE OF PHARMACY,SILVASSA JIDNESH DHARMAMEHER
METHODS OF PREPARATION
Solvent extraction:
It is a non-aqueous method of microencapsulation, particularly
suitable for water labile polymers such as the polyanhydrides.
In this method, drug is dispersed or dissolved in a solution of the
selected polymer in a volatile organic solvent like methylene chloride.
This mixture is then suspended in silicone oil containing Span 85 and
methylene chloride.
After pouring the polymer solution into silicone oil, petroleum ether
is added and stirred until solvent is extracted into the oil solution. The
resulting microspheres can then be dried in vacuum.
15. 20SSRMPH06 SSR COLLEGE OF PHARMACY,SILVASSA JIDNESH DHARMAMEHER
METHODS OF PREPARATION
Solvent extraction:
16. 20SSRMPH06 SSR COLLEGE OF PHARMACY,SILVASSA JIDNESH DHARMAMEHER
METHODS OF PREPARATION
HYDROGEL MICROSPHERE:
Microspheres made of gel-type polymers, such as alginate, are
produced by dissolving the polymer in an aqueous solution,
suspending the active ingredient in the mixture and extruding
through a precision device, producing microdroplets which fall into a
hardening bath, that is slowly stirred.
The hardening bath usually contains calcium chloride solution,
whereby the divalent calcium ions crosslink the polymer forming
gelled microspheres. The method involves an all-aqueous” system
and avoids residual solvents in microspheres.
The surface of these microspheres can be further modified by coating
them with polycationic polymers, like polylysine after fabrication. The
particle size of microspheres can be controlled by using various size
extruders or by varying the polymer solution flow rates.
17. 20SSRMPH06 SSR COLLEGE OF PHARMACY,SILVASSA JIDNESH DHARMAMEHER
METHODS OF PREPARATION
HYDROGEL MICROSPHERE:
18. 20SSRMPH06 SSR COLLEGE OF PHARMACY,SILVASSA JIDNESH DHARMAMEHER
METHODS OF PREPARATION
SPRAY DRYING:
This was used to prepare polymeric blended microsphere loaded with
drug.
It involves dispersing the core material into liquefied coating material
and then spraying the mixture in the environment for solidification of
coating followed by rapid evaporation of solvent.
Organic solution of poly (epsilon-caprolactone) (PCL) and cellulose
acetate butyrate (CAB), in different weight ratios and drug were
prepared and sprayed in different experimental condition achieving
drug loaded microspheres.
• The quality of spray-dried microspheres can be improved by the
addition of plasticizers, e.g. citric acid, which promote polymer
coalescence on the drug particles and hence promote the formation
of spherical and smooth surfaced microspheres.
19. 20SSRMPH06 SSR COLLEGE OF PHARMACY,SILVASSA JIDNESH DHARMAMEHER
METHODS OF PREPARATION
SPRAY DRYING:
The size of microspheres can be controlled by the rate of spraying,
the feed rate of polymer drug solution, nozzle size, and the drying
temperature.
This method of microencapsulation is particularly less dependent on
the solubility characteristics of the drug and polymer and is simple,
reproducible, and easy to scale up
It is widely used method for preparation of the microspheres.
20. 20SSRMPH06 SSR COLLEGE OF PHARMACY,SILVASSA JIDNESH DHARMAMEHER
METHODS OF PREPARATION
SPRAY DRYING:
21. 20SSRMPH06 SSR COLLEGE OF PHARMACY,SILVASSA JIDNESH DHARMAMEHER
METHODS OF PREPARATION
PHASE INVERSION MICROENCAPSULATION:
The process involves addition of drug to a dilute solution of the
polymer (usually 1–5%, w/v in methylene chloride).
The mixture is poured into an unstirred bath of a strong non-solvent
(petroleum ether) in a solvent to non-solvent ratio of 1:100, resulting
in the spontaneous production of microspheres through phase
inversion.
The microsphere in the size range of 0.5–5.0 m can then be filtered,
washed with petroleum ether and dried with air.
This simple and fast process of microencapsulation involves relatively
little loss of polymer and drug.
22. 20SSRMPH06 SSR COLLEGE OF PHARMACY,SILVASSA JIDNESH DHARMAMEHER
METHODS OF PREPARATION
PHASE INVERSION MICROENCAPSULATION:
23. 20SSRMPH06 SSR COLLEGE OF PHARMACY,SILVASSA JIDNESH DHARMAMEHER
METHODS OF PREPARATION
ALKALINE CO-PRECIPITATION:
Treat poly (acrylic acid–divinylbenzene) microspheres with dilute
aqueous NaOH solution (0.5 M) for hours at suitable temperature to
transform the carboxylic acid groups to sodium carboxylates and then
washed thoroughly with water to remove the excess NaOH till neutral
pH.
• Purged the microsphere suspension with nitrogen for 30 min. To this
suspension add an aqueous solution of FeCl3 and FeCl2 that had been
purged with nitrogen.
• Stirred the mixture overnight under nitrogen atmosphere for ion
exchange.
24. 20SSRMPH06 SSR COLLEGE OF PHARMACY,SILVASSA JIDNESH DHARMAMEHER
METHODS OF PREPARATION
ALKALINE CO-PRECIPITATION:
The resulting microspheres were washed repeatedly with water
under nitrogen atmosphere to remove excess iron salts.
Added drop wise an aqueous NaOH solution (3 M) to a suspension of
the microspheres taken up with iron ions under nitrogen atmosphere
to adjust the pH value to be >12. The mixture was then heated to 60
°C and kept for another 2 h.
The resulting magnetic microspheres were suspended in an aqueous
HCl solution (0.1 M) to transform the –COONa to –COOH, and then
washed thoroughly with water to neutral pH, dried under vacuum at
50 °C overnight, giving magnetic microspheres.
25. 20SSRMPH06 SSR COLLEGE OF PHARMACY,SILVASSA JIDNESH DHARMAMEHER
METHODS OF PREPARATION
ALKALINE CO-PRECIPITATION:
26. 20SSRMPH06 SSR COLLEGE OF PHARMACY,SILVASSA JIDNESH DHARMAMEHER
METHODS OF PREPARATION
INVERSE PHASE SUSPENSION POLYMERIZATION:
A 250 mL three-neck flask fitted with a mechanical stirrer used for
performing the reaction.
Continuous phase includes: 100 mL of castor oil and 10 mL of span
80. Determined amount of itaconic acid (IA), Styrene (St),
divinylbenzene (DVB) and N, N_ Methylene-bisacrylamide (BIS)
dissolved completely in DMSO, and the organic phase was added
drop wisely into the flask, with 70 °C heating using an oil bath.
Ammonium persulfate (INITIATOR) added The reaction proceeded for
8 h with continuous stirring. The resulting microspheres were
separated by centrifugation. Further washed with diethyl ether and
then by deionized water.
27. 20SSRMPH06 SSR COLLEGE OF PHARMACY,SILVASSA JIDNESH DHARMAMEHER
METHODS OF PREPARATION
SONOCHEMICAL METHOD:
Decane and iron pentacarbonyl Fe(CO)5 were layered over a 5% w/v
protein solution(BSA).
The bottom of the high-intensity ultrasonic horn was positioned at
the aqueous organic interface.
The mixture was irradiated for 3 min, employing a power of W150 W/
32cm with the initial temperature of 23 °C in the reaction cell. The pH
was adjusted to 7.0 by adding HCl.
This procedure was performed again with an aqueous solution of iron
acetate, Fe(CH3CO2)2.
28. 20SSRMPH06 SSR COLLEGE OF PHARMACY,SILVASSA JIDNESH DHARMAMEHER
METHODS OF PREPARATION
SONOCHEMICAL METHOD:
After the synthesis, the products were separated from the unreacted
protein and from the residues of iron acetate or iron pentacarbonyl
by centrifugation (1 000 r/min for 5 min).
The magnetic microspheres were washed a few times with sufficient
volumes of water to remove the residues
.
29. 20SSRMPH06 SSR COLLEGE OF PHARMACY,SILVASSA JIDNESH DHARMAMEHER
METHODS OF PREPARATION
• Spray Cooling/ Chilling:
Spray cooling/chilling is the least expensive encapsulation
technology.
It is used for the encapsulation of organic and inorganic salts,
textural ingredients, enzymes, flavors and other functional
ingredients.
It improves heat stability, delay release in wet environments,
and/or convert liquid hydrophilic ingredient into free flowing
powders.
Spray cooling/chilling is typically referred to as ‘matrix’
encapsulation because the particles are more adequately
described as aggregates of active ingredient particles buried in
the fat matrix.
31. 20SSRMPH06 SSR COLLEGE OF PHARMACY,SILVASSA JIDNESH DHARMAMEHER
PAN COATING
1. Solid particles are mixed with a dry coating
material.
2. The temperature is raised so that the coating
material melts and encloses
3. the core particles, and then is solidified by
cooling.
32. 20SSRMPH06 SSR COLLEGE OF PHARMACY,SILVASSA JIDNESH DHARMAMEHER
PAN COATING
Or,
the coating material can be gradually applied to
core particles tumbling in a vessel rather than
being wholly mixed with the core particles from
the start of encapsulation.
https://www.slideshare.net/GajananSanap/microencapsulation-58778836
33. 20SSRMPH06 SSR COLLEGE OF PHARMACY,SILVASSA JIDNESH DHARMAMEHER
PAN COATING
The particles are tumbled in a pan or
other device while the coating
material is applied slowly
The coating is applied as a solution
or as an atomized spray to the
desired solid core material in the
coating pan
Usually, to remove the coating
solvent, warm air is passed over the
coated materials as the coatings are
being applied in the coating pans.
In some cases, final solvent removal
is accomplished in drying oven.
34. 20SSRMPH06 SSR COLLEGE OF PHARMACY,SILVASSA JIDNESH DHARMAMEHER
Different methods and polymers
.
Process used Polymers
Comments
Particle size
(µm)
Polymers used
Solvent evaporation 1-100 Relatively stable polymers,
e.g.
polyesters, polystyrene
Hot melt
microencapsulation
1-1000 Water labile polymers, e.g.
polyanhydrides,
polyesters;
with a molecular weight of
1000-50000
Solvent removal 1-300 High melting point
polymers
especially polyanhydrides
Spray drying 1-10 Polylactide (PLA) and
polylactide-co-glycolide
(PLGA) were mostly used
Phase inversion 0.5-5 Chitosan, CMC,
alginate,polyanhydride
J.K.
Vasir
et al
35. 20SSRMPH06 SSR COLLEGE OF PHARMACY,SILVASSA JIDNESH DHARMAMEHER
• CORE MATERIAL:
It is a specific material to be coated which can be solid/liquid.
Liquid core: oil,dispersion,solution.
Solid core: API, stabilizer,diluent or any excipient.
• Coating material:
It is material which can form film or envolope around core
material.
MATERIALS USED IN PRPARATION OF MICROSPHERES
36. 20SSRMPH06 SSR COLLEGE OF PHARMACY,SILVASSA JIDNESH DHARMAMEHER
It should be capable of forming film which is
cohesive with core material.
Material should be satisfy product objective and
reuirement.
Best suited for the method of encapsulation.
SELECTION CRITERIA FOR COATING MATERIAL
37. 20SSRMPH06 SSR COLLEGE OF PHARMACY,SILVASSA JIDNESH DHARMAMEHER
1. Stabilization of core material.
2. Inert toward active ingredients.
3. Controlled release under specific conditions.
4. Film-forming, pliable, tasteless, stable.
5. Non-hygroscopic, no high viscosity, economical.
6. Soluble in an aqueous media or solvent, or
melting.
7. The coating can be flexible, brittle, hard, thin etc.
IDEAL PROPRTIES FOR COATING MATERIAL
https://www.slideshare.net/GajananSanap/microencapsulation-58778836
38. 20SSRMPH06 SSR COLLEGE OF PHARMACY,SILVASSA JIDNESH DHARMAMEHER
Classification of polymers
POLYMERS
SYNTHETIC NATURAL
Non
biodegra
dable
biodegradable
CARBOHYDRATES
PROTEIN
Chemically
modified
carbohydrates
39. 20SSRMPH06 SSR COLLEGE OF PHARMACY,SILVASSA JIDNESH DHARMAMEHER
Material used Types Examples
Synthetic polymers a) Biodegradable
b) Non biodegradable
Glycosides,epoxy polymer
Poly
anhydride,lacticides,acrotein,glycidyl
methylacryl
Natural a) Carbohydrates
b) Protein
c) Chemically modified
carbohydrate
Agarose,starch,chitosan etc.
Gelatin,albumin,collagen etc.
Polydextran,polystarch etc.
Satinder Kakar et al.
40. 20SSRMPH06 SSR COLLEGE OF PHARMACY,SILVASSA JIDNESH DHARMAMEHER
TYPES OF MICROSPHERES
MICROSPHERES
BIOADHESIVE
MAGNETIC
DIAGNOSTIC
THERAPEUTIC
FLOATING
raadioactive
41. 20SSRMPH06 SSR COLLEGE OF PHARMACY,SILVASSA JIDNESH DHARMAMEHER
1.BIOADHESIVE MICROSPHERES:
Bioadhesive microspheres include microparticles and microcapsules
(having a core of the drug) of 1–1000µm in diameter and consisting
either entirely of a bioadhesive polymer or having an outer coating of
it, respectively.
Microspheres, in general, have the potential to be used for targeted
and controlled release drug delivery; but coupling of bioadhesive
properties to microspheres has additional advantages, e.g. efficient
absorption and enhanced bioavailability of the drugs due to a high
surface to volume ratio, a much more intimate contact with the
mucus layer, specific targeting of drugs to the absorption site
achieved by anchoring plant lectins, bacterial adhesins and
antibodies, etc. on the surface of the microspheres.
.
TYPES OF MICROSPHERES
42. 20SSRMPH06 SSR COLLEGE OF PHARMACY,SILVASSA JIDNESH DHARMAMEHER
1.BIOADHESIVE MICROSPHERES:
Bioadhesive microspheres can be tailored to adhere to any mucosal
tissue including those found in eye, nasal cavity, urinary and
gastrointestinal tract, thus offering the possibilities of localised as
well as systemic controlled release of drugs.
.
TYPES OF MICROSPHERES
43. 20SSRMPH06 SSR COLLEGE OF PHARMACY,SILVASSA JIDNESH DHARMAMEHER
1.BIOADHESIVE MICROSPHERES:
The specific mucosal surfaces can be targeted using site-specific
chemical agents that are anchored onto the polymeric DDS. The first
generation mucoadhesive polymers lack specificity and can bind to
any mucosal surface.
.
TYPES OF MICROSPHERES
44. 20SSRMPH06 SSR COLLEGE OF PHARMACY,SILVASSA JIDNESH DHARMAMEHER
1.BIOADHESIVE MICROSPHERES:
TYPES OF MICROSPHERES
No Glycosyl groups on
cell membranes
Specific ligands Specific site
1 Mannose Galanthus nivalis
agglutinin (GNA)
Epithelial cells in stomach,
caecum, and colon
2 N-Acetyl glucosamine Wheat germ
agglutinin (WGA)
Epithelial cells in stomach,
caecum, colon and
absorptive enterocytes in small
intestine
3 N-Acetyl
galactosamine
Lectin ML-1 from
Viscum album
Endocytosed by villus enterocytes
and goblet cells
Strong binding to epithelial cells in
small intestine
4 Fucose Aleuria aurentia
agglutinin (AAA)
Specific binding and transcytosis
by M cells
J.K. Vasir et al.
45. 20SSRMPH06 SSR COLLEGE OF PHARMACY,SILVASSA JIDNESH DHARMAMEHER
1.BIOADHESIVE MICROSPHERES:
Some mechanism involved in bioadhesion:
1.electrostatic force of attraction.
2. adsorption – Surface forces resulting in chemical bonding.
3. wetting: Ability of bioadhesive polymers to spread and develop
intimate contact with the mucus membranes.
4. Diffusion theory: Physical entanglement of mucin strands and the
flexible polymer chains.
TYPES OF MICROSPHERES
J.K. Vasir et al.
46. 20SSRMPH06 SSR COLLEGE OF PHARMACY,SILVASSA JIDNESH DHARMAMEHER
1.BIOADHESIVE MICROSPHERES:
• Methods of preparation:
Solvent evaporation
Hot melt microencapsulation
Solvent extraction
Hydrogel microspheres
Spray drying
Phase inversion
TYPES OF MICROSPHERES
47. 20SSRMPH06 SSR COLLEGE OF PHARMACY,SILVASSA JIDNESH DHARMAMEHER
• APPLICATIONS:
TYPES OF MICROSPHERES
DRUG ROUTE OF ADMINISTRATION POLYMER USED COMMENTS
ACYCLOVIR Ocular Chitosan Slow release rate and increase AUC
Methyl prednisolone Ocular Hyaluronic acid Slow release rates
Sustained drug concentration in tear fluids
Gentamicin Nasal DSM + LPC Increased nasal absorption
Insulin Nasal DSM + LPC Efficient delivery of insulin into the
systemic
circulation via nasal route
Amoxicillin GI AD-MMS (PGEFs) Greater anti H. pylori activity
Riboflavin GI AD-MMS (PGEFs) Higher AUC
Effective absorption from the absorption
window
Nerve growth factor
(nGF)
Vaginal HYAFF Increased absorption from HYAFF microspheres
Vancomycin Colonic PGEF coated with Eudragit
S 100
Well absorbed even without absorption
enhancers
Insulin Colonic PGEF coated with Eudragit
S 100
Absorbed only in the presence of absorption
enhancers, e.g. EDTA salts
J.K.
Vasir
et
al.
48. 20SSRMPH06 SSR COLLEGE OF PHARMACY,SILVASSA JIDNESH DHARMAMEHER
2.MAGNETIC MICROSPHERES:
• Magnetic drug delivery by particulate carriers is an efficient method
of drug delivery to a localized disease site.
• A drug or therapeutic radioisotope is encapsulated in a magnetic
compound; injected into patient’s blood stream & then stopped with
a powerful magnetic field in the target area.
• Drug targeting is a specific form of drug delivery where the drug is
directed to its site action or absorption.
TYPES OF MICROSPHERES
49. 20SSRMPH06 SSR COLLEGE OF PHARMACY,SILVASSA JIDNESH DHARMAMEHER
2.MAGNETIC MICROSPHERES:
Two different types of magnetic microspheres:
1. Therapeutic magnetic microspheres:
It is used to deliver chemotherapeutic agent to liver tumor. Drugs like
proteins and peptides can also be targeted through this system.
2. Diagnostic magnetic microspheres:
It can be used for imaging liver metastases and also can be used to
distinguish bowel loops from other abdominal structures by forming
nano size particles supramagnetic iron oxides.
TYPES OF MICROSPHERES
50. 20SSRMPH06 SSR COLLEGE OF PHARMACY,SILVASSA JIDNESH DHARMAMEHER
MAGNETIC MICROSPHERE
Representation of systemic drug delivery and magnetic drug delivery
51. 20SSRMPH06 SSR COLLEGE OF PHARMACY,SILVASSA JIDNESH DHARMAMEHER
MAGNETIC MICROSPHERE
Magnetic drug targeting.
52. 20SSRMPH06 SSR COLLEGE OF PHARMACY,SILVASSA JIDNESH DHARMAMEHER
2.MAGNETIC MICROSPHERES:
Material used in preparation of magnetic microspheres:
TYPES OF MICROSPHERES
53. 20SSRMPH06 SSR COLLEGE OF PHARMACY,SILVASSA JIDNESH DHARMAMEHER
• Methods of preparation:
• Phase inversion
• Alkaline co-precipitation
• Inverse phase sepration polymerization
• Sono chemical
MAGNETIC MICROSPHERES
54. 20SSRMPH06 SSR COLLEGE OF PHARMACY,SILVASSA JIDNESH DHARMAMEHER
• APPLICATIONS:
MAGNETIC MICROSPHERES
No Application Carrier/drug
1 Tumor targeting Mitoxantrone, Paclitaxel
2 Radioembolisation of liver and spleen tumors 186re/188re-glass
Microspheres
3 Magnetic bioseparation Dynabeads, used in
isolation of mRNA, genomic
DNA and proteins
4 Bacteria detection Streptavidin coated
magnetic beads
5 Contraceptive drug delivery Drug delivery is designed to
change in steroid secretion
during menstrual cycle.
55. 20SSRMPH06 SSR COLLEGE OF PHARMACY,SILVASSA JIDNESH DHARMAMEHER
Floating microspheres are gastro-retentive drug delivery
systems based on non-effervescent approach.
Hollow microspheres are in strict sense, spherical empty
particles without core.
These microspheres are characteristically free flowing
powders consisting of proteins or synthetic polymers,
ideally having a size less than 200 μm.
Due to its small particle size, these are widely distributed
throughout the gastrointestinal tract which improves drug
absorption and reduces side effects due to localized buildup
of irritating drugs against the gastrointestinal mucosa.
FLOATING MICROSPHERES
56. 20SSRMPH06 SSR COLLEGE OF PHARMACY,SILVASSA JIDNESH DHARMAMEHER
METHODS OF PREPARATION:
• Solvent evaporation
• Co-acervation phase sepration
• Ionotropic gelation method
FLOATING MICROSPHERES
57. 20SSRMPH06 SSR COLLEGE OF PHARMACY,SILVASSA JIDNESH DHARMAMEHER
POLYMER USED AND ITS APPLICATION:
FLOATING MICROSPHERES
DRUG ROUTE OF
ADMINISTRATION
POLYMER USED USE
Amoxicillin GI Ethyl cellulose-Carbopol-
934P
Greater anti H. pylori
activity
Delapril HCl GI Polyglycerol esters of fatty
acids (PGEFs)
MRT of drug is increased
Glipizide GI Chitosan Prolonged blood glucose
reduction
Glipizide GI Chitosan-alginate Prolonged blood glucose
reduction
Furosemide GI Polyglycerol esters of fatty
acids (PGEFs)
Increased bioavailability
Higher AUC
effective absorption from
the absorption
window.
www.globalresearchonline.net
58. 20SSRMPH06 SSR COLLEGE OF PHARMACY,SILVASSA JIDNESH DHARMAMEHER
Radio embolization therapy microspheres sized 10-30 nm are of
larger than the diameter of the capillaries and gets tapped in first
capillary bed when they come across.
They are injected in the arteries that leads them to tumour of interest
so all these conditions radioactive microspheres deliver high radiation
dose to the targeted areas without damaging the normal surrounding
the targeted areas without damaging the normal surrounding tissue.
It differs from drug delivery system, as radio activity is not released
from microspheres but acts from within a radioisotope typical
distance and the different kinds of radioactive microspheres are α
emitters, β emitters, γ emitters.
The effective treatment range in tissue is up to about 90 μm (10 cell
layers) for α -emitters, never more than 12 mm for β-emitters
and up to several centimetres for γ -emitters.
RADIOACTIVE MICROSPHERES
M. De Cuyper and J.W.M. Bulte
59. 20SSRMPH06 SSR COLLEGE OF PHARMACY,SILVASSA JIDNESH DHARMAMEHER
METHOD OF PREPARATION:
RADIOLABELING DURING THE MICROSPHERE PREPARATION:
RADIOACTIVE MICROSPHERES
Method of Labelling Examples
Colloid precipitation 99mTc sulphur colloid, 113mIn ferric hydroxide colloids,
165Dy-FHMA (~5 μm),
Isotope exchange 14C-, 35S- and 3H-labeling
Lipophilic inclusion 186Re/1 88Re-triphenylphosphine-liposomes
In situ production 99mTc-Buckminster fullerenes (C60 or C80) or aggregates
thereof (Technegas)
60. 20SSRMPH06 SSR COLLEGE OF PHARMACY,SILVASSA JIDNESH DHARMAMEHER
METHOD OF PREPARATION:
RADIOLABELING AFTER THE MICROSPHERE PREPARATION:
RADIOACTIVE MICROSPHERES
Method of Labelling Examples
Radiolabelling by ion
exchange
Anion- and cation-exchange resins:
BioRex 70 loaded with 90Y
Dowex 1-X4 loaded with 99mTcO4-
Dowex I-X8 loadedwith 56CrO4
Affinity to microsphere
material
153Sm-citrate bound to hydroxyapatite
microspheres
Reduction to insoluble,
colloidal compounds
99mTc-Sn PLA microspheres
61. 20SSRMPH06 SSR COLLEGE OF PHARMACY,SILVASSA JIDNESH DHARMAMEHER
APPLICATIONS:
DIAGNOSTIC APPLICATIONS:
RADIOACTIVE MICROSPHERES
Application Type of radioactive
microspheres used
Particle size
Infection localisation 111In-labeled leukocytes
111In-labeled liposomes
99mTc-labeled liposomes
99mTc-albumin
nanocolloid
12-20 μm
20 nm-1 μm
20 nm-1 μm
<80 nm
Tumour imaging 99mTc-labeled liposomes
67Ga-NTA
20 nm- 1 μm
65 nm
Gastrointestinal transit
studies
99m Tc-sulfur colloid 0.05-0.6 μm
62. 20SSRMPH06 SSR COLLEGE OF PHARMACY,SILVASSA JIDNESH DHARMAMEHER
APPLICATIONS:
THERAPEUTICS APPLICATIONS:
RADIOACTIVE MICROSPHERES
Application Type of radioactive
microspheres used
Particle size
Local radiotherapy 90Y-labeled poly(lactic
acid)
165Dy-acetylacetone
poly(lactic acid)
1-5 or 10-50 µm
1-5 or 10-50 µm
Intracavitary treatment
(peritoneal ovarian
tumour, metastases, cystic
brain tumour)
chromic 32P-phosphate
90Y-silicate, 90Y-citrate
198Au suspensions
1-2 μm
0.01-1 μm
5-25 nm
63. 20SSRMPH06 SSR COLLEGE OF PHARMACY,SILVASSA JIDNESH DHARMAMEHER
• Particle size and shape:
Method used:
light microscopy:
LM provides a control over coating parameters
in case of double walled microspheres. The microspheres
structures can be visualized before and after coating and
the change can be measured microscopically.
EVALUATION
Alagusundaram.M. et al /Int.J. ChemTech
Res.2009,1(3)
64. 20SSRMPH06 SSR COLLEGE OF PHARMACY,SILVASSA JIDNESH DHARMAMEHER
• Particle size and shape:
Method used:
Scanning electron microscopy:
SEM provides higher resolution in contrast to the
LM. SEM allows investigations of the microspheres
surfaces and after particles are cross-sectioned, it can also
be used for the investigation of double walled systems.
EVALUTION
65. 20SSRMPH06 SSR COLLEGE OF PHARMACY,SILVASSA JIDNESH DHARMAMEHER
Electron spectroscopy for chemical analysis:
The surface chemistry of the microspheres can
be determined using the electron spectroscopy for
chemical analysis (ESCA). ESCA provides a means for
the determination of the atomic composition of the
surface. The spectra obtained using ECSA can be used to
determine the surfacial degradation of the biodegradable
microspheres.
EVALUTION
66. 20SSRMPH06 SSR COLLEGE OF PHARMACY,SILVASSA JIDNESH DHARMAMEHER
• Infrared Spectroscopy:
FT-IR is used to determine the degradation of the
polymeric matrix of the carrier system. The surface of the
microspheres is investigated measuring alternated total
reflectance (ATR). The IR beam passing through the
ATR cell reflected many times through the sample to
provide IR spectra mainly of surface material. The ATRFTIR
provides information about the surface composition
of the microspheres depending upon manufacturing
procedures and conditions.
EVALUTION
67. 20SSRMPH06 SSR COLLEGE OF PHARMACY,SILVASSA JIDNESH DHARMAMEHER
• DENSITY DETERMINATION:
Using multivolume pycnometer.
Helium is exposed and allowed for expansion.
Two consecutive readings of reduction in pressure at different
initial pressure are noted.
From two pressure readings the volume and hence the density of the
microsphere carrier is determined.
EVALUTION
68. 20SSRMPH06 SSR COLLEGE OF PHARMACY,SILVASSA JIDNESH DHARMAMEHER
Solid state by DSC/XRD:
This test is done to find out the solid state property of the
drug and polymers used in the prparation of the
microspheres.
EVALUTION
DSC
XRD
Satinder Kakar et al.
69. 20SSRMPH06 SSR COLLEGE OF PHARMACY,SILVASSA JIDNESH DHARMAMEHER
• Isoelectric point:
The micro electrophoresis is an apparatus used to measure
the electrophoretic mobility of microspheres from which
the isoelectric point can be determined.
mean velocity at different Ph values ranging from 3-10 is
calculated by measuring the time of particle movement
over a distance of 1 mm.
By using this data the electrical mobility of the particle can
be determined.
EVALUTION
Alagusundaram.M. et al /Int.J. ChemTech
Res.2009,1(3)
70. 20SSRMPH06 SSR COLLEGE OF PHARMACY,SILVASSA JIDNESH DHARMAMEHER
• Capture efficiency:
Encapsulation efficiency was calculated using the formula:
Encapsulation efficiency =
(Actual Drug Content / Theoretical Drug Content) ×100
• Estimation of Drug Content:
Weight equivalent to drug is measure and then analysis is
done by uv spectroscopic method.
EVALUTION
71. 20SSRMPH06 SSR COLLEGE OF PHARMACY,SILVASSA JIDNESH DHARMAMEHER
IN VITRO DISSOLUTION :
BEAKER METHOD:
The dosage form in this method is made to adhere at the bottom of
the beaker containing the medium and stirred uniformly using over
head stirrer. Volume of the medium used in the literature for the
studies varies from 50-500 ml and the stirrer speed form 60-300 rpm.
Modified Keshary Chien Cell:
It comprised of a Keshary Chien cell containing distilled water (50ml)
at 370 C as dissolution medium. TMDDS (Trans Membrane Drug
Delivery System) was placed in a glass tube fitted with a 10# sieve at
the bottom which reciprocated in the medium at 30 strokes per min.
EVALUTION
72. 20SSRMPH06 SSR COLLEGE OF PHARMACY,SILVASSA JIDNESH DHARMAMEHER
IN VITRO DISSOLUTION :
• Dissolution apparatus:
Standard USP or BP dissolution apparatus have been used
to study in vitro release profiles using both rotating
elements, paddle and basket Dissolution medium used for
the study varied from 100- 500 ml and speed of rotation
from 50-100 rpm.
EVALUTION
73. 20SSRMPH06 SSR COLLEGE OF PHARMACY,SILVASSA JIDNESH DHARMAMEHER
Ophthalmic Drug Delivery
Oral drug delivery
Gene delivery
Nasal drug delivery
Intratumoral and local drug delivery
Buccal drug delivery
Gastrointestinal drug delivery
Transdermal drug delivery
Colonic drug delivery
Vaginal drug delivery
Targeting by using microparticulate carriers
Cosmetics
APPLICATIONS
Kadam N. R. and Suvarna V.:
75. 20SSRMPH06 SSR COLLEGE OF PHARMACY,SILVASSA JIDNESH DHARMAMEHER
FDA Approved products
Vivian Saez et al.
76. 20SSRMPH06 SSR COLLEGE OF PHARMACY,SILVASSA JIDNESH DHARMAMEHER
FDA Approved products
• Rykindo is approved by USFDA in march 2019
• Recently it is launched by Luye pharma in china
in the month of march 2021.
Alzhimer
disease
https://www.luye.cn/lvye_en/view.php?id=1890
77. 20SSRMPH06 SSR COLLEGE OF PHARMACY,SILVASSA JIDNESH DHARMAMEHER
MARKETED FORMULATIONS
Drug Commercial Name Company Technology
Risperidone RISPERDAL®
CONSTA®
Janssen®/Alkerme
s
Double emulsion
(oil in water)
Naltrexone Vivitrol Alkermes Double emulsion
(oil in water)
Leuprolide Trenantone® Takeda Double emulsion
(oil in water)
Octreotide Sandostatin® LAR Novartis Phase separation
Minocycline Arestin® Orapharma -
Triptorelin Trelstar™ depot Pfizer Phase separation
Lanreotide Somatuline® LA Ipsen-Beafour Phase separation
Bromocriptine Parlodel LAR ™ Novartis Spray drying
https://www.researchgate.net/publication/281405531_MICROSPHERES_A_RECENT_UP
DATE/download
79. 20SSRMPH06 SSR COLLEGE OF PHARMACY,SILVASSA JIDNESH DHARMAMEHER
MARKETED FORMULATIONS
OXYBENZONONE
SUNSCREEN
80. 20SSRMPH06 SSR COLLEGE OF PHARMACY,SILVASSA JIDNESH DHARMAMEHER
PATENTS
No Patent No. Drug used
1 CN 201110142359 Ketoprofen
2 CN 201110313846 Paclitaxel
3 CN 201210025085 5-fluorouracil
4 US08455091 Ganciclovir
5 EP19980924438 Cimetidine
6 EP20070808011 Risperidone
7 CA 2217462 Cyclosporin
8 CA 2579533 Irinotecan
9 DE1999609777 Levonorgesterel
10 DE1994632867 Doxorubicin
https://w
ww.resea
rchgate.n
et/figure
/Patents-
of-
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eres_tbl2
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81. 20SSRMPH06 SSR COLLEGE OF PHARMACY,SILVASSA JIDNESH DHARMAMEHER
PATENTS
J.K. Vasir et al.
82. 20SSRMPH06 SSR COLLEGE OF PHARMACY,SILVASSA JIDNESH DHARMAMEHER
RECENT ADVANCEMENT
Verma et al
83. 20SSRMPH06 SSR COLLEGE OF PHARMACY,SILVASSA JIDNESH DHARMAMEHER
RECENT ADVANCEMENT
Verma et al
84. 20SSRMPH06 SSR COLLEGE OF PHARMACY,SILVASSA JIDNESH DHARMAMEHER
In future by combining various other strategies,
microspheres will find the central place in novel
drug delivery, particularly in diseased cell sorting,
diagnostics, gene & genetic materials, safe,
targeted and effective in vivo delivery and
supplements as miniature versions of diseased
organ and tissues in the body.
FUTURE APPROACH
85. 20SSRMPH06 SSR COLLEGE OF PHARMACY,SILVASSA JIDNESH DHARMAMEHER
Microspheres have been appeared as effective controlled release
dosage forms and represents great pharmaceutical applications in
area of drug delivery technology with multidisciplinary
advancements for treatment of number of diseases.
Microspheres because of their attractive properties in terms of
patient compliance, therapeutic efficacy, and reduction in side
effects these delivery systems provide various therapeutic
benefits over conventional dosage forms. There is further place
for improvement in future in microsphere drug delivery systems
for more therapeutic results.
Combination of microparticles with different novel strategies
particularly in diagnostic area, diseased cell sorting, entrapment
of genetic materials and tissue engineered products within the
matrix.
CONCLUSION
86. 20SSRMPH06 SSR COLLEGE OF PHARMACY,SILVASSA JIDNESH DHARMAMEHER
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drug delivery system. International Journal of Pharmaceutics , 255, 13-32.
2. Satinder Kakar, D. B. (2013). Magnetic microspheres as magical novel drug
delivery system: A review. Journal of Acute Disease , 1-12.
3. Solanki, N. (2018). Microspheres an innovative approach in drug delivery
system. MOJ Bioequivalence & Bioavailability , 5 (1), 56-58
4. HÄFELI, U. (2001). RADIOACTIVE MICROSPHERES FOR MEDICAL
APPLICATIONS. Physics and Chemistry Basis ofBiotechnology , 213-248.
5. Prasad, B. S. (2014). MICROSPHERES AS DRUG DELIVERY SYSTEM – A REVIEW.
Journal of Global Trends in Pharmaceutical Sciences , 5(3), 1961-1972.
6. Prashant Singh, T. g. (2011). Biodegradable Polymeric Microspheres as Drug
Carriers; A Review. Indian Journal of Novel Drug Delivery , 3(2), 70-82.
7. Nirav R. Patel, D. A. (2011). Microsphere as a novel drug delivery.
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REFERENCES
87. 20SSRMPH06 SSR COLLEGE OF PHARMACY,SILVASSA JIDNESH DHARMAMEHER
8.Harsh Bansal, S. P. (2011). MICROSPHERE: METHODS OF PREPRATION AND
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