Microencapsulation is a process where tiny particles or droplets of a core material are surrounded by a coating to form capsules in the micrometer to millimeter range called microcapsules. Various techniques are used to produce microcapsules including air suspension, pan coating, coacervation, solvent evaporation, and polymerization. Microencapsulation offers advantages like taste masking, sustained release, and protection of materials. Microcapsules find applications in pharmaceuticals for controlled drug delivery and replacement of non-oral therapeutics. Some commercial products that use microencapsulation technology include Lupin Cefadroxil, ZORprin CR, and Glipizide SR.
Easy & to the point Topics are clearly given in this presentation..
Thanks & Best Regard
(Anurag Pandey) B.Pharm
Contact :- anurag.dmk05@gmail.com (Facebook & Gmail both)
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.
SOLID DISPERSION
Definition: The technology is the science of dispersing one or more active ingredients in an inert matrix in the solid stage.
Need of solid dispersion:
Increases Oral bioavailability of a drug
Increased dissolution rate.
Enhanced release of drugs from ointment.
Improved the solubility & stability.
The concept of solid dispersion was originally proposed by Sekiguchi & obi.
Increasing the dissolution, absorption & therapeutic efficacy of drugs in dosage forms.
Increasing solubility in water.
Improving the oral absorption and bioavailability of BCS Class II drugs.
“It is define has an substance or Pharmaceutical material is encapsulated over the surface of solid, droplet of liquid and dispersion of medium is known has Microencapsulation”
Video Lecture is available at https://www.youtube.com/watch?v=DXu_CLgB4q0
Introduction, terminology/definitions and rationale, advantages, disadvantages, selection of drug candidates. Approaches to design-controlled release formulations based on diffusion, dissolution and ion exchange principles. Physicochemical and
biological properties of drugs relevant to controlled release formulations.
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
Gastro retentive drug delivery system (GRDDS)Shweta Nehate
Oral route is the most acceptable route for drug administration. Apart from conventional dosage forms several other forms were developed in order to enhance the drug delivery for prolonged time period and for delivering drug to a particular target site. Gastro-retentive drug delivery system (GRDDS) has gainned immense popularity in the field of oral drug delivery recently. it is a widely employed approach to retain the dosage form in the stomach for an extended period of time and release the drug slowly that can address many challenges associated with conventional oral delivery, including poor bioavailability. different innovative approaches are being applied to fabricate GRDDS. Gastroretentive drug delivery is an approach to prolong gastric residence time, there by targeting site-specific drugs release in the upper gastrointestinal tract (GIT) for local or systemic effects. It is obtained by retaining dosage form into stomach and by releasing the in controlled manner.
"Capsula" is derived from the Latin word & Is defined as a solid dosage form in which the medicament contained is enclosed within small shell or container.
Easy & to the point Topics are clearly given in this presentation..
Thanks & Best Regard
(Anurag Pandey) B.Pharm
Contact :- anurag.dmk05@gmail.com (Facebook & Gmail both)
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.
SOLID DISPERSION
Definition: The technology is the science of dispersing one or more active ingredients in an inert matrix in the solid stage.
Need of solid dispersion:
Increases Oral bioavailability of a drug
Increased dissolution rate.
Enhanced release of drugs from ointment.
Improved the solubility & stability.
The concept of solid dispersion was originally proposed by Sekiguchi & obi.
Increasing the dissolution, absorption & therapeutic efficacy of drugs in dosage forms.
Increasing solubility in water.
Improving the oral absorption and bioavailability of BCS Class II drugs.
“It is define has an substance or Pharmaceutical material is encapsulated over the surface of solid, droplet of liquid and dispersion of medium is known has Microencapsulation”
Video Lecture is available at https://www.youtube.com/watch?v=DXu_CLgB4q0
Introduction, terminology/definitions and rationale, advantages, disadvantages, selection of drug candidates. Approaches to design-controlled release formulations based on diffusion, dissolution and ion exchange principles. Physicochemical and
biological properties of drugs relevant to controlled release formulations.
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
Gastro retentive drug delivery system (GRDDS)Shweta Nehate
Oral route is the most acceptable route for drug administration. Apart from conventional dosage forms several other forms were developed in order to enhance the drug delivery for prolonged time period and for delivering drug to a particular target site. Gastro-retentive drug delivery system (GRDDS) has gainned immense popularity in the field of oral drug delivery recently. it is a widely employed approach to retain the dosage form in the stomach for an extended period of time and release the drug slowly that can address many challenges associated with conventional oral delivery, including poor bioavailability. different innovative approaches are being applied to fabricate GRDDS. Gastroretentive drug delivery is an approach to prolong gastric residence time, there by targeting site-specific drugs release in the upper gastrointestinal tract (GIT) for local or systemic effects. It is obtained by retaining dosage form into stomach and by releasing the in controlled manner.
"Capsula" is derived from the Latin word & Is defined as a solid dosage form in which the medicament contained is enclosed within small shell or container.
microencapsulation is the part of an pharmaceutics, in that the method of preperation is giving. and all related thing about microencapsulation is given.
thanks you.
2. DEFINITION
Microencapsulation is the
process by which tiny solid
particles or droplets of
liquid are surrounded or
coated with a continuous
film of polymeric material to
produce capsules in the
micrometer to millimeter
range. The product obtained
by this process is called as
microcapsules.1
Microcapsule
4. Advantages of microencapsulation
Masking of bitter taste drugs. Eg: Ofloxacin.
Conversion of liquid to pseudo solid.
Eg: Eprazinone.2
Environmental protection.
Eg: Vit.A.Palmitate.
Reduction of hygroscopicity .Eg: NaCl.
Reduction of vaporization of volatile drugs.
Eg: Methyl salicylate.
Prevention of incompatibilities among drugs.
Eg: Aspirin and Chlorpheniramine maleate .2
5. Disadvantages of Microencapsulation.
Possible cross reaction between core and
shell material.
Difficult to achieve continuous and uniform
film.
Shelf life of hygroscopic drugs is
reduced.
More production costs.
More skill and knowledge is required.2
6. MECHANISMS OF DRUG RELEASE
Degradation
controlled
monolithic
system
Diffusion
controlled
monolithic
system
Diffusion
controlled
reservoir
system
Erosion
7. MECHANISMS OF DRUG RELEASE
1)Degradation controlled monolithic
system-Drug releases on degradation
of matrix.
2)Diffusion controlled monolithic
system-Drug released by diffusion
then degradation of matrix occurs.
3)Diffusion controlled reservoir
system-Drug from capsule diffuses
then rate controlling membrane
erodes.
4)Erosion-Due to pH and enzymatic
hydrolysis.2
9. MATERIALS INVOLVED IN FORMULATION
A)Core Material:
Specific material to be coated.
It may be liquid or solid.
Liquid core may be dissolved or dispersed
material.3
10. Core Material Purpose Final
Product
Form
Acetaminophen Taste masking Tablet
Potassium
chloride
Reduces
gastric
irritation
Capsule
Isosorbide
dinitrate
Sustained
release
Capsule
Examples of core material
11. B)Coating Material: Inert substance
which coats on core with desired
thickness.
Composition of coating solution
•Inert polymer.
•Plasticizer- Triethylcitrate, glycerin
•Solvents- Water,cyclohexane.
•Co solvents-Glycerol, sorbitol.
12. Examples of various coating material 3
Category of Coating
Material
Examples
Water soluble resins Gelatin,
Polyvinylpyrrolidone(PVP).
Water insoluble resins Ethyl cellulose, Polyethylene.
Waxes and lipids Paraffin, Carnauba, Beeswax.
Enteric resins Shellac, Zein.
13. TECHNIQUES TO MANUFACTURE
MICROCAPSULES
S.No Physical Methods Chemical Methods
A) Air Suspension Solvent Evaporation
B) Pan Coating Polymerization
C) Coarcervation Phase
Separation
Interfacial
Polymerization
In-situ PolymerizationD) Multi-orifice
Centrifugal Process
E) Spray Drying & Spray
Congealing
F) Fluidized Bed
Technology
14. A)Air Suspension(Wurster Method)
Within the coating chamber, particles are
suspended on an upward moving air stream.
Spraying of coating material on the air suspended
particles.
The cyclic process is repeated depending upon
purpose of microencapsulation.
Air stream serves to dry the product.3
16. B) Pan Coating
The particles are tumbled in a pan while
the coating material is applied slowly as
solution or atomized spray to the core.
To remove the coating solvent, warm air is
passed over the coated materials or dusting
of talc is done.
17. Medicaments are usually coated onto
nonpareil sugar seeds and then coated with
polymers.3
Advantages: Disadvantages:
Suitable to
larger particles.
Time consuming.
Sustained
release
preparations.
High material
loss.
18. C) Coacervation Phase Separation:
Simple coacervation Complex coacervation
A desolvation agent is
added for phase separation
It involves complexation
between two oppositely
charged polymers.
Steps involved in this process are:-
1)Formation of three immiscible phases.
2)Deposition of liquid coating material upon
the core material.
3)Rigidization of coating.
20. Various methods to obtain three immiscible phases:
1) Temperature change
2) Incompatible Polymer Addition
3) Non-Solvent Addition
4) Salt Addition
5) Polymer-Polymer Interaction(Complex Coacervation)
21. Temperature change:
Temperature-composition
phase diagram for a binary
system of a polymer and a
solvent.
TEMPERATURE
POLYMER CONCENTRATION %
X
A
B
C D
E
F G
•Point X represents –single phase.
The phase-boundary curve indicates
that with decreasing temperature.
One phase
becomes
polymer rich.
Other phase
becomes polymer
poor.
Eg: N-acetyl p-amino phenol.4
22. Non-Solvent Addition:
A liquid that is a non-solvent
for a given polymer can be added to
a solution of the polymer to induce
phase separation.
Eg: Addition of isopropyl ether to
CAB dissolved in methyl ethyl
ketone.
Core: Methyl scopolamine HBr.4
A
B
C
D
E
SOLVENT
100%
100%
POLYMER
100%
NON
SOLVENT
Phase diagram for
phase-separation/
coacervation induced by
Non Solvent Addition
23. Salt Addition
Soluble inorganic salts can
be added to aqueous
solutions of water-soluble
polymers .
Eg: Sodium sulfate,
Core-Vitamin in corn oil.4
25. D) Multi-orifice Centrifugal Process
Advantages:
Encapsulates both solid and liquid materials.
Production rate is more.
It utilizes centrifugal forces to hurl a core material particle
through an enveloping microencapsulation membrane .4
27. Spray Drying Spray Congealing
Coating solidification
effected by rapid
evaporation of solvent in
which coating material is
dissolved.
Coating solidification is
effected by thermally
congealing a molten
coating material.4
Advantages:
Low bulk density product.
Porous nature capsules.
Free flowing particles.
30. NOVEL METHODS
A) Vibration Technology
A fluid stream of liquid
core and shell materials
is pumped through
concentric tubes and
forms droplets under the
influence of vibration. 1
31. B) Jet Cutter Technology
A solid jet of fluid coming out of a nozzle by means of
rotating cutting wires is cut into cylindrical segments
which then form beads due to surface tension on their way
to a hardening device.1
32. C) Rapid Expansion Of Super Critical
Solution(RSS)
Core and the shell material are maintained at high pressure
and then released at atmospheric pressure through a small
nozzle.
Sudden drop in pressure causes desolvation of the shell
material.1
33. APPLICATIONS
To reduce gastric and other GIT irritations.
Eg: Aspirin preparations.
Prolonged release dosage forms preparation.
Preparation of enteric-coated dosage forms .
Replacement of therapeutic agents (not taken
orally like insulin), gene therapy and in use of
vaccines for treating AIDS, tumors, cancer and
diabetes.
Delivery of DNA vaccines.
Prodrug approach. Eg: Minocycline HCl.
Biodegradable and biocompatible microparicles
preparations.Example: Risperidone or testosterone.5
34. Marketed formulations prepared using
microcapsules5
S.No Brand
Name
Generic
Name
Category
of drug
1. Lupin Cefadroxil Antibiotic
2. ZORprin CR Aspirin Anti-arthritic
3. Glipizide SR Glucotrol Anti diabetic
35. REFERENCES
1. http://www.authorstream.com/Presentation/vivekchauhan-
1147305-microencapsulation.
2. Hammad umer et.al,” International Journal of Research in
Pharmaceutical and Biomedical Sciences” ISSN: 2229-
3701.
3. S. S. Bansode et.al,” Institute of Pharmaceutical Education
And Research”, Volume 1, Issue 2, March –April 2010;
Article 008 .
4. Lachman LA, Liberman HA, Kanig JL. The Theory and
Practice of Industrial Pharmacy. Mumbai, India: Varghese
Publishing House; 3:414-415.
5. http://www.authorstream.com/Presentation/thokesagar-
1295371-shree/