MICROENCAPSULATI

ON
Prepared by : Tejas J. Patel
Associate Professor
Department of Pharmaceutics
SNLPCP, Umrakh.
 INTRODUCTION:
• Microparticles are defined as the polymeric
entities falling in the range of 1-1000
micrometer.
• It covers two types of forms:
1) Microcapsule: Micrometric reservoir system.
2) Microsphere: Micrometric matrix system.
• Microcapsule: It contain an active agent and it
surrounded by polymeric shell or coating material
and dispersed in polymeric reservoir.
• Microsphere are small spherical particles made
up of polymeric substances, in which the drug is
dispersed through out the microsphere matrix with
diameter in the micrometers range.
• Microbeads are alternative terms of microsphere.
• MICROENCAPSULATION is a process by
which very tiny droplets or particles of liquid
or solid material are surrounded or coated
with a continuous film of polymeric material.
• The product obtained by this process is
called as Microcapsules.
• Their diameters generally range from a few
microns to a few millimetres.
• Generally Microcapsule consist of two
components
a) Core material.
b) Coat or wall or shell material.
a) Core material: The material to be coated. It may
be liquid or solid or gas. Liquid core may be
dissolved or dispersed material. Composition of
core material:
Drug or active constituent
Additive like diluents
Stabilizers.
b) Coating Material : Inert substance which coats
on core with desired thickness. Composition of
coating:
Inert polymer
Plasticizer
Coloring agent
Resins, waxes and lipids
Release rate enhancers or retardants
REASONS FOR ENCAPSULATION :
The core must be isolated from its
surroundings, as
1. To protect reactive substances from the
environment,
2. To convert liquid active components into a
dry solid system,
3. To separate incompatible components for
functional reasons,
4. To protect the immediate environment of the
microcapsules from the active components.
 ADVANTAGES
• Shelf life may be Increased.
• Do not interfere with other ingredients.
• Wider range of products for consumer to
choose from.
• Sensory properties remain unaltered.
• Can be added anytime in processing &
remains unaltered.
• Food production have increased health
benefits.
• Consumer would not get taste of added
capsules.
 DISADVANTAGES
• More skill and knowledge is required to
use this technology.
• Production Cost is High.
• Difficult to achieve continuous and
uniform film.
• Possible cross reaction may occur in
wall and material selected.
• Shelf life of hygroscopic drug is
reduced.
• Due to Foreign ingredient customer
with allergies may face problems.
RELEASE MECHANISM
⦿ A variety of release mechanisms have
been proposed for microcapsule:
1) By pressure or shear stress.
2) By melting the wall.
3) By solvent action.
4) By enzyme attack.
5) By chemical reaction.
6) By hydrolysis or slow disintegration.
METHOD OF
MICROENCAPSULATION
Microencapsulation
Techniques

Physical or physico-
Physico-chemical Chemical
mechanical

1. Air Suspension 1. Ionotropic gelation 1. Solvent-Evaporation

2. Centrifugal Extrusion 2. Coacervation 2. Polymerization
3. Pan coating 2.1 Interfacial polymer
4. Spray drying 2.2 In-situ polymer
5. Vibrational nozzle 2.3 Matrix polymer
A] Physical or Physico-mechanical
methods
1. Air-suspension :
Inventions of Professor Dale E. Wurster
Basically the wurster process consists of the
dispersing of solid, particulate core materials in a
supporting air stream and the spray-coating of the
air suspended particles.
Equipment ranging in capacities from one
pound to 990 pounds.
Micron or submicron particles can be effectively
encapsulated by air suspension techniques.
Disadvantage- Agglomeration of the particles to
some larger size is normally achieved.
 Processing variables for efficient, effective
encapsulation by air suspension techniques:
1.Density, surface area, melting point, solubility,
friability, volatility, Crystallinity, and flow-ability
of core material.
2.Coating material concentration (or melting
point if not a solution).
3.Coating material application rate.
4.Volume of air required to support and fluidizes
the core material.
5.Amount of coating material required.
6.Inlet and outlet operating temperatures.
❑ Solid, particulate core material are dispersed in
a supporting air stream.
❑ The coating material is sprayed on the air
suspended particles.
❑ Within the coating chamber, particles are
suspended on an upward moving air stream.
❑ The design of the chamber and its operating
parameter effect a recalculating flow of the
particles through the coating zone portion of the
chamber, where a coating material usually a
polymer solution, is spray applied to the moving
particles.
❑ The supporting air stream also serves to dry the
product while it is being encapsulated.
2. Centrifugal extrusion :
❑ It is a mechanical process for producing
microcapsule.
❑ Centrifugal force are used to hurl a core
material particle through an enveloping
microencapsulation membrane.
Liquids are encapsulated using a rotating
extrusion head containing concentric nozzles.
This process is excellent for forming particles
400–2,000 μm in diameter.
 Since the drops are formed by the breakup of a
liquid jet, the process is only suitable for liquid or
slurry.
 A high production rate can be achieved, i.e.,
50 to 75 pounds pr hour have been
achieved with this process.
Heads containing 16 nozzles are available.
❑ This process is capable for
microencapsulating liquids and solids of
varied size ranges with diverse coating
materials.
❑ It is currently used by some vitamin
manufacturers for the encapsulation of
Vitamin A.
3. Pan coating :
Oldest industrial procedures for forming small,
coated particles or tablets.
The particles are tumbled in a pan or other
device while the coating material is applied
slowly.
Solid particles greater than 600 microns in
size are generally considered essential for
effective coating.
Medicaments are usually coated onto various
spherical substrates such as nonpareil sugar
seeds, and then coated with protective layers
of various polymers.
❑ It is used for preparation of controlled
release beads.
❑ Coating is applied as solution by atomized
spray to desired solid core material in
coating pan.
❑ Usually warm air is passed over the coated
material as the coating are being applied in
the coating pan.
4. Spray-drying:
In modern spray dryers the viscosity of the
solutions to be sprayed can be as high as
300mPa.s
Spray drying and spray congealing- dispersing
the core material in a liquefied coating
substance and spraying.
Spray drying is effected by rapid evaporation of
a solvent in which the coating material is
dissolved.
The equipment components of a standard
spray dryer include:
1. An air heater, 2. Atomizer,
3. Main Drying chamber, 4. Exhaust fan,
5. Cyclone and 6. Collection vessel.
 Spray congealing can be accomplished with
spray drying equipment when the protective
coating is applied as a melt.
Core material is dispersed in a coating material
melt rather than a coating solution.
Coating solidification (and microencapsulation)
is accomplished by spraying the hot mixture into
a cool air stream.
Airflow :There are three modes of contact:
1. Co-current
2. Counter-current
3. Mixed-flow
5. Vibrational Nozzle :
The process works very
well for generating droplets
between 100–5,000 µm.
Units are deployed in
industries and research
mostly with capacities of
1–10,000 kg per hour at
working temperatures of
20–1500 C.
Nozzles heads are
available from one up to
several hundred thousand
are available.
❑ Core-shell encapsulation can be done using
a laminar flow through a nozzle and an
additional vibration of the nozzle or the liquid.
❑ The liquid can consist of any liquids with
limited viscosities (0 to 10,000 mPa.s) e.g.
Solutions, suspensions, emulations, melts
etc.
❑ The solidification can be done according to
the used gelation system with an internal
gelation. (e.g. Sol-gel processing) or an
external. (additional binder system e.g. In a
slurry)
B] Physico-chemical
methods
1. Ionotropic gelation:
Chemical reaction between sodium alginate
and calcium chloride or other Counter ion
solution such as barium chloride.
Verapamil hydrochloride causes gastric
irritation on sudden release. It is usually
administered as conventional tablets
containing 40-120 mg, 3 times a day. Due to
its ready solubility in water and shorter half-
life.
Micro particulate system of verapamil
hydrochloride for prolonged release delivery
system.
2. Coacervation-Phase Separation:
❑ Microencapsulation by coacervation phase
separation is generally attributed to The
National Cash Register (NCR) Corporation and
the patents of B.K. Green et al.
❑ The process consists of three steps:
Formation of three immiscible phases; a
liquid manufacturing phase, a core material
phase and a coating material phase.
Deposition of the liquid polymer coating on
the core material.
Rigidizing the coating usually by thermal,
cross linking or desolvation techniques to form
a microcapsule.
❑ In step 2, the deposition of the liquid polymer
around the interface formed between the core
material and the liquid vehicle phase.
❑ In many cases physical or chemical changes in the
coating polymer solution can be induced so that
phase separation of the polymer will occur.
❑ Droplets of concentrated polymer solution will form
and coalesce to yield a two phase liquid-liquid
system. In cases in which the coating material is an
immiscible polymer of insoluble liquid polymer it
may be added directly.
❑ Also monomers can be dissolved in the liquid
vehicle phase and subsequently polymerized at
interface.
❑ Equipment required for microencapsulation this
method is relatively simple; it consists mainly of
jacketed tanks with variable speed agitators .
C] Chemical process
1. Solvent Evaporation :
In this method the core material is dispersed or
dissolved in the polymer solution, polymer
shrinks around the core. After evaporation a
matrix - type microcapsule is formed.
The core materials may be either,
water - soluble or water - insoluble materials.
A variety of film - forming polymers can be used
as coatings.
E.g. Evaluation of Sucrose Esters as Alternative
Surfactants in Microencapsulation of Proteins by
the Solvent Evaporation Method.
2. Polymerization :
a) Interfacial polymer : In Interfacial polymerization,
the two reactants in a polycondensation meet at an
interface and react rapidly.
b) In-situ polymerization : In a few microencapsulation
processes, the direct polymerization of a single
monomer is carried out on the particle surface.
e.g. Cellulose fibers are encapsulated in
polyethylene while immersed in dry toluene. Usual
deposition rates are about 0.5μm/min. Coating
thickness ranges 0.2-75μm.
c) Matrix polymer : In a number of processes, a core
material is imbedded in a polymeric matrix during
formation of the particles. Prepares microcapsules
containing protein solutions by incorporating the
protein in the aqueous diamine phase.
APPLICATIONS
• To mask bitter taste of drugs like Paracetamol,
Nitrofurantoin.
• Reduce gastric and other G.I. tract irritations.
• A liquid can be converted to a pseudo-solid for
easy handling and storage. eg.Eprazinone.
• Hygroscopic properties of core materials may
be reduced by microencapsulation eg. Sodium
chloride.
• To reduce odor and volatility.
• To provide protection to the core materials
against atmospheric effects, e.g.Vit.A.Palmitate.
• Separation of incompatible substance. e.g.
pharmaceutical eutectics.
• Sustained release. e.g. Aspirin.
• To improve the flow properties e.g. Thiamine.
• To enhance the stability e.g. Vitamin
• In gene therapy and In use of vaccines for
treating AIDS, tumors, cancer and diabetes.
• Microencapsulation has also been used to
decrease potential danger of handling of toxic or
noxious substances. e.g. Fumigants, herbicides,
insecticides and pesticides
Thank You