This document discusses microparticulate drug delivery systems. It defines microparticles as particles ranging from 1 micron to a few millimeters that can encapsulate drugs. Microparticles provide benefits like protecting drugs from the environment, sustained drug release, and targeted delivery. The document discusses microparticle morphology, important features, advantages, disadvantages, applications, release mechanisms, preparation techniques including emulsion polymerization, and factors influencing encapsulation. It concludes that these delivery systems offer benefits over conventional dosage forms like improved efficacy, reduced toxicity, and patient compliance.
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
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
‘Targeted drug delivery system is a special form of drug delivery system where the medicament is selectively targeted or delivered only to its site of action or absorption and not to the non-target organs or tissues or cells.’
“Microparticles are defined as particulate dispersions or solid particles with a size in the range of 1-1000 μm.”
The drug is dissolved, entrapped, encapsulated or attached to a microparticle matrix.
Application Of Polymer In Controlled Release FormulationAnindya Jana
Polymers are becoming increasingly important in the field of drug delivery. The pharmaceutical applications of polymers range from their use as binders in tablets to viscosity and flow controlling agents in liquids, suspensions and emulsions. Polymers can be used as film coatings to disguise the unpleasant taste of a drug, to enhance drug stability and to modify drug release characteristics.
As a consequence, increasing attention has been focused on methods of giving drugs continually for a prolonged time periods and in a controlled fashion.
This technology now spans many fields and includes pharmaceutical, food and agricultural applications, pesticides, cosmetics, and household products.
‘Targeted drug delivery system is a special form of drug delivery system where the medicament is selectively targeted or delivered only to its site of action or absorption and not to the non-target organs or tissues or cells.’
“Microparticles are defined as particulate dispersions or solid particles with a size in the range of 1-1000 μm.”
The drug is dissolved, entrapped, encapsulated or attached to a microparticle matrix.
Application Of Polymer In Controlled Release FormulationAnindya Jana
Polymers are becoming increasingly important in the field of drug delivery. The pharmaceutical applications of polymers range from their use as binders in tablets to viscosity and flow controlling agents in liquids, suspensions and emulsions. Polymers can be used as film coatings to disguise the unpleasant taste of a drug, to enhance drug stability and to modify drug release characteristics.
As a consequence, increasing attention has been focused on methods of giving drugs continually for a prolonged time periods and in a controlled fashion.
This technology now spans many fields and includes pharmaceutical, food and agricultural applications, pesticides, cosmetics, and household products.
Content:
Introduction
Ideal Properties
Advantages
Limitations
Types of Microsphere
Method for Preparation
Polymer Used for Preparation
Release of Drug from Microsphere
Application
magnetic microspheres a noval drug delivery system in this we are learn about microshperes , magnetic microsphere and preparation method of magnetic microsphere.
In this presentation incude method of preparation ,evaluvation of magnetic microspheres and concept of targeting.
Polymer microspheres for controlled drug releaseDuwan Arismendy
Polymer microspheres can be employed to deliver medication in a rate-controlled and sometimes targeted manner. Medication is released from a microsphere by drug leaching from the polymer or by degradation of the polymer matrix. Since the rate of drug release is controlled by these two factors, it is important to understand the physical and chemical properties of the releasing medium. This review presents the methods used in the preparation of microspheres from monomers or from linear polymers and discusses the physio-chemical properties that affect the formation, structure, and morphology of the spheres. Topics including the effects of molecular weight, blended spheres, crystallinity, drug distribution, porosity, and sphere size are discussed in relation to the characteristics of the release process. Added control over release profiles can be obtained by the employment of core-shell systems and pH-sensitive spheres; the enhancements presented by such systems are discussed through literature examples.
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microparticulate drug delivery system ppt
1. “MICROPARTICULATE DRUG
DELIVERY SYSTEM”
“Microparticulate drug delivery system”
Dissertation submitted to Rajasthan University of Health
Sciences, Jaipur, in the partial fulfillment of the
requirements
For the degree of BACHELOR OF PHARMACY
Submitted by
Student Name : ISHFAQ AHMAD RATHER
Roll. No: 413017
B.PHARMACY PART- IV
(Enrollment No. 2012 /1071 )
Under the Guidance of
(Supervisor Name) : Mr. GURPREET SINGH
Qualification : M.Pharma , Ph.D*
Désignation : Asst.professor (pharmaceutics)
2. CONTENTS
(1) INTRODUCTION
MORPHOLOGY OF MICROPARITCLE
IMPORTANT FEATURES OF
MICROCAPSULES
ADVANTAGES
DISADVANTAGES
(2) APPLICATIONS Microparticulate
(3) RELEASE MECHANISM
(4) CARRIERS USED IN
PREPARATION OF
MICROPARTICLES
FACTORS INFLUENCING
ENCAPSULATION
(5) EVALUATION OF
MICROPARTICLES:
(6) CONCLUSION
3. MICROPARTICULATE DRUG
DELIVERY SYSTEM
INTRODUCTION
ORAL DRUG ADMINISTRATION IS BY FAR THE MOST
PREFERABLE ROUTE FOR TAKING MEDICATIONS.
HOWEVER, THEIR SHORT CIRCULATING HALF LIFE AND
RESTRICTED ABSORPTION VIA A DEFINED SEGMENT OF
INTESTINE LIMITS THE THERAPEUTIC POTENTIAL OF
MANY DRUGS.
4. MICROPARTICLES
MICROPARTICLES ARE A TYPE OF DRUG DELIVERY
SYSTEMS WHERE THE PARTICLE SIZE RANGES
FROM ONE MICRON (ONE THOUSANDTH OF A MM)
TO FEW MM. THIS MICROENCAPSULATION
TECHNOLOGY ALLOWS PROTECTION OF DRUG
FROM THE
ENVIRONMENT,
STABILIZATION OF SENSITIVE DRUG
SUBSTANCES,
ELIMINATION OF INCOMPATIBILITIES, OR
MASKING OF UNPLEASANT TASTE.
5. MORPHOLOGY OF MICROPARITCLE
Microencapsulation is a technology
used to entrap solids, liquids, or
gases inside a polymeric matrix or
shell. Microparticles are :
Microcapsule is a system in which drug
containing core is completely
surrounded by a polymer shell. .
Microsphere is a system in which the drug
substance is either homogenously
dissolved or dispersed in a polymeric
matrix.
6. IMPORTANT FEATURES OF
MICROCAPSULES
The most significant feature of microcapsules is
their microscopic size that allows for a huge
surface area, The total surface area is
inversely proportional to the diameter. This
large surface area is available for sites of
adsorption and desorption, chemical
reactions, .
ADVANTAGES This type of drug delivery
systems mainly provides the encapsulated
material to reach the area of action without
getting adversely affected by the environment
through which it passes. Pharmaceutical and
biomedical advantages of microparticle
include:
1. Taste and odor masking.
2. . Protection of drugs from environment.
3. 3. Particle size reduction for enhancing
solubility of the poorly soluble drug
4. . 4. Sustained or controlled drug delivery Eg:
KCl, Ibuprofen.
5. 5. Targeted release of encapsulated
material. .
7. DISADVANTAGES
:
1. The costs of the materials and processing of
the controlled release preparation, which
may be substantially higher than those of
standard formulations.
2. . Process conditions like change in
temperature, pH, solvent addition, and
evaporation/agitation may influence the
stability of core particles to be encapsulated.
3. The environmental impact of the
degradation products of the polymer matrix
produced in response to heat, hydrolysis,
oxidation, solar radiation or biological
agents .
8. RELEASE MECHANISM
l Generally there are three different
mechanisms by which the core
material is released from a
microcapsule
Mechanical rupture of the capsule
wall
Dissolution or melting of the wall
and
Diffusion through the wall .
Diffusion: On contact with aqueous
fluids in the gastrointestinal tract
(GIT), water diffuses into the
interior of the particle. Drug
dissolution occurs and the drug
9. TECHNIQUES OF
MICROENCAPSULATION:
A variety of techniques are employed for the
entrapment of solids or liquids
The preparation method can be broadly
divided into 2 categories:
Chemical methods and
physical methods.
Chemical Methods This method uses
monomers/prepolymers as starting
materials. These methods involve
chemical reactions along with microsphere
formation. These include
suspension polymerization, emulsion
polymerization, dispersion and interfacial
methods.
Among them emulsion polymerization
method is widely used in drug delivery
10. Emulsion Polymerization According to
this technique the monomer is added
drop wise to the stored aqueous
polymerization medium containing the
material to be encapsulated () and a
suitable emulsifier. The polymerization
begins and initially produced polymer
molecules precipitate in the aq. medium
to form primary nuclei. As the
polymerization proceeds, these nuclei
grow gradually and simultaneously
entrap the core material to form the final
microcapsules as shown in figure.
12. Figure: 11. schematic representation of the coacervation process.(a) core material dispersion in solution of shell polymer; (b)separation of coacervate from solution; (c) coating of corematerial by microdroplets of coacervate; (d) coalescence of
14. ,CONCLUSION
. These delivery systems offer numerous
advantages compared to conventional
dosage forms, which include
Efficacy,
Reduced toxicity, and
Improved patient compliance
..
Although toxicity problems may exist, they will
be resolved by modifying the factors that
influence these systems.
15. REFERENCES
1. Gattani YS. Floating Multiparticulate drug delivery
systems: An overview International Journal of
Pharma and Biosciences, 6(2), 2010, 35-40.
2. Rama Dubey, Shamc TC and Bhaskar Rao KV.
Microencapsulation technology and applications.
Defense Science Journal, 59(1), 2009, 82-83.
3. Edith Mathiowitz, Mark R.Kreitz, Lisa Brannon-
Peppas. Microencapsulation. Outline, 5(2), 2008,
495-496.
4. Frederic Jewes, Frank Boury, Jean-Pierre Benoit
Inserm U 646, Ingenierie Da La Vectorisation
Particulaire, Universite D Angers, France.
Biodegradable microspheres: Advances in
production technology: Microencapsulation:
methods and industrial applications. Second
edition, 158, 1988, 1-23.
5. Kinam Park, Yoon Yeo. Microencapsulation
technology encyclopedia of pharmaceutical
technology GEPT, 6(2), 2002, 67-85.
6. James Swar Brick, James E. Boylan, Mercel
dekkar. Microencapsulation technology and
applications. Encyclopedia of pharmaceutical
Technology,10, 1988, 245-286.