A
Presentation
On
MICROENCAPSULATION
By Under the guidance of
SANA TABASSUM Mrs.Ch.S VIJAYA VANI,M.Pharm .
Associate Professor,
(B.Pharm) Department of Pharmaceutics.
CMR COLLEGE OF PHARMACY
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
MICROCAPSULES
Microscopic view Microcapsules in
of microcapsules blood stream
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
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
MECHANISMS OF DRUG RELEASE
Degradation Diffusion Diffusion Erosion
controlled controlled controlled
monolithic monolithic reservoir
system system system
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
CLASSIFICATION OF MICROCAPSULES2
Mononuclear Polynuclear Matrix Mononuclear
with
multiple
shells
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
Examples of core material
Core Material Purpose Final
Product
Form
Acetaminophen Taste masking Tablet
Potassium Reduces Capsule
chloride gastric
irritation
Isosorbide Sustained Capsule
dinitrate release
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 .
Examples of various coating material 3
Category of Coating Examples
Material
Water soluble resins Gelatin,
Polyvinylpyrrolidone(PVP).
Water insoluble resins Ethyl cellulose, Polyethylene.
Waxes and lipids Paraffin, Carnauba, Beeswax.
Enteric resins Shellac, Zein.
TECHNIQUES TO MANUFACTURE
MICROCAPSULES
S.No Physical Methods Chemical Methods
A) Air Suspension Solvent Evaporation
B) Pan Coating Polymerization
C) Coarcervation Phase Interfacial
Separation Polymerization
D) Multi-orifice In-situ Polymerization
Centrifugal Process
E) Spray Drying & Spray
Congealing
F) Fluidized Bed
Technology
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
Advantages: Disadvantages:
Various Applicable only
coating to solid core
material can be material.
used.
Capacity is Agglomeration
more of the particles
WURSTER APPARATUS
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.
Medicaments are usually coated onto
nonpareil sugar seeds and then coated with
polymers.3
Advantages: Disadvantages:
Suitable to Time consuming.
larger particles.
Sustained High material
release loss.
preparations.
C) Coacervation Phase Separation:
Simple coacervation Complex coacervation
A desolvation agent is It involves complexation
added for phase separation 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.
Coacervation process
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)
Temperature change:
•Point X represents –single phase. A
XE
The phase-boundary curve indicates
TEMPERATURE
that with decreasing temperature.
C D
B
One phase F G
Other phase POLYMER CONCENTRATION %
becomes becomes polymer Temperature-composition
polymer rich. poor. phase diagram for a binary
system of a polymer and a
Eg: N-acetyl p-amino phenol.4 solvent.
Non-Solvent Addition: SOLVENT
100%
A liquid that is a non-solvent A
for a given polymer can be added to
E
a solution of the polymer to induce D
phase separation. B
C
Eg: Addition of isopropyl ether to
CAB dissolved in methyl ethyl 100%
NON 100%
ketone. SOLVENT POLYMER
Core: Methyl scopolamine HBr.4 Phase diagram for
phase-separation/
coacervation induced by
Non Solvent Addition
Salt Addition
Soluble inorganic salts can
be added to aqueous
solutions of water-soluble
polymers .
Eg: Sodium sulfate,
Core-Vitamin in corn oil.4
Polymer-Polymer Interaction (Complex WATER
Coacervation): 100%
A
Steps involved:4
XC
1. Formation of an O/W emulsion
B
2. Formation of the coating
3. Stabilization of the coating
100% 100
%
P+
P -
Ternary Phase
diagram
D) Multi-orifice Centrifugal Process
It utilizes centrifugal forces to hurl a core material particle
through an enveloping microencapsulation membrane .4
Advantages:
Encapsulates both solid and liquid materials.
Production rate is more.
E) Spray Drying and Spray Congealing:
Spray Drying Spray Congealing
Coating solidification Coating solidification is
effected by rapid effected by thermally
evaporation of solvent in congealing a molten
which coating material is coating material.4
dissolved.
Advantages:
Low bulk density product.
Porous nature capsules.
Free flowing particles.
F) Solvent Evaporation
Advantages:
Encapsulation of hydrophobic and hydrophilic drug.
Simple technique.
Encapsulation of solid and liquid drug.
G) Polymerization
Interfacial Polymerization In-situ Polymerization
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
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
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
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
Marketed formulations prepared using
microcapsules5
S.No Brand Generic Category
Name Name of drug
1. Lupin Cefadroxil Antibiotic
2. ZORprin CR Aspirin Anti-arthritic
3. Glipizide SR Glucotrol Anti diabetic
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/
