MICROENCAPSULATION

DR. S. VIDYADHARA
Professor & Principal
CHIPS
o Micro encapsulation is the means of applying thin
coatings to small particles of solids or droplets of liquids
and dispersions. The coating of particles ranging from
several tenths of a micron to 5000 microns in size.

o Microencapsulation provides the means of converting

the liquids to solids, of altering the colloidal and surface
properties, of providing environmental protection,
ADVANTAGES:

o Microencapsulation provides the means of converting

liquids to solids.

o Altering colloidal and surface properties.

o Providing environmental protection

o Controlling the release characteristics.

DISADVANTAGES:

o No single microencapsulation process is adaptable to all core

material candidates or product applications.

o Difficulties such as incomplete or discontinuous coating

o Inadequate stability or shelf life of sensitive pharmaceuticals.

o Non reproducible and unstable release characteristics of coated

products

o Economic limitations often are encountered in the attempt to

apply particular microencapsulation method.
➢ Fundamental Considerations:

✓ Core Material:

o The core material, defined as the specific material to

be coated , can be liquid or solid in nature.

o The solid core can be a mixture of active

constituents , stabilizers , diluents, excipients, and
accelerants.
Coating Material:

The selection of a specific coating material depends upon that

o What are the specific dosage or product requirements- stabilization,

reduced volatility, release characteristics , environmental conditions.

o What coating material will satisfy the product objectives and

requirements.

o What microencapsulation method is best suited to accomplish the

coated product objectives.
o The coating material should be capable of forming a film that
is cohesive with the core material, be chemically compatible
and non reactive with the core material and provide a desired
coating properties, such as strength, flexibility, impermeability,
optical properties, and stability.

o The typical coating properties such as cohesiveness ,

permeability,moisture sorption, solubility, stability and clarity
must be considered in the selection of the proper
microcapsule coating material.
➢ Selected Stability , Release And Other Properties:

% of
potency
Remainin
g

Days at 450 c & 75% R.H

Stability of microencapsulated vitamin A palmitate corn oil prepared by

Phase separation or coacervation technique compared with unencapsulated control
 a. Aspirin hydrolysis of
chlorpheniramine
maleate- aspirin mixture

b. Aspirin hydrolysis of
microencapsulated mixture.

c. Hydrolysis of aspirin
control.

Stability enhancement of
incompatible aspirin mixture
by microencapsulation
The above graph shows that the stability of microencapsulated
Volatile liquids, prepared by coacervation phase separation
Invitro release patterns of crystalline aspirin coated with
various amounts of ethyl cellulose using phase separation
coacervation techniques.
EQUPMENT AND PROCESSING:
o Air suspension.

o Coacervation phase separation.

o Multi orifice-centrifugal process.

o Spray drying and congealing

o Pan Coating.

o Solvent evaporation techniques.

o Polymerization.
 a. Control panel

b. Coating chamber.

c. Particles being treated.

d. Process air flow.

e. Air distribution plate.

f. Nozzle for applying film

WURSTER AIR SUSPENSION
coatings.
APPARATUS
Processing variables that receive consideration for efficient ,
effective, encapsulation by air suspension include:

o Density, surface area, melting point, solubility, friability, volatility ,

crystallinity and flowability to the core material.

o Coating material concentration.

o Coating material application rate.

o Volume of air required to support and fluidize the core material.

o Amount of coating material required.

o Inlet and outlet operating temperatures.

Coacervation Phase Separation:

o Microencapsulation by coacervation phase separation is generally

attributed to The National Cash Register (NCR) The process
consists of three steps

o Formation of three immiscible phases; a liquid manufacturing

phase, a core material phase and a coating material phase.

o Deposition of the liquid polymer coating on the core material.

o Rigidizing the coating usually by thermal, cross linking or

desolvation techniques to form a microcapsule.
STEP
-I
o To form the three phases, the
core material is dispersed in a
solution of coating polymer, the
solvent for the polymer being
the liquid manufacturing
vehicle phase.
o The coating material phase, an
immiscible polymer in a liquid
state, is formed by utilizing one
of the methods of phase
separation coacervation i.e. by
changing temperature of
polymer solution or by adding
the salt, non solvent, or
incompatible polymer to the
polymer solution.
STEP-
II

The deposition of the liquid

polymer around the
interface formed between
the core material and the
liquid vehicle phase.

.
STEP-
III

This process involves

rigidizing the coating ,
usually by thermal, cross

linking, or desolvation
techniques, to form self
sustaining microcapsule.
➢ Temperature Changes:

➢ Ex:N – Acetyl Para Aminophenol coated with EC

dissolved in cyclohexane as solvent.
➢ Incompatible Polymer Addition:

Four Parts of Methylene Blue HCl is coated with

two % EC dissolved in toluene is phase separated
by the addition of 25 parts of incompatible
polymer Polybutadiene
➢ Non Solvent Addition:

Methyscopolamine Hydrobromide is coated with 5

% W/V of CAB dissolved in methylethyl ketone is
phase separated by the addition of 1:2 parts of
isopropyl ether as non solvent
 ➢ Salt Addition:

Vitamin A in corn oil is emulsified with 10% Gelatin at 500c is

microencapsulated by adding 20% Sodium sulphate as salt solution
which is further rigidized by transferring them in to 7% sodium
sulphate solution at 190C
➢ Polymer- Polymer Interaction:
25 % of Methyl
100% water Salicylate is
emulsified by
interacting
positively charged
2% Gelatin with
negatively charged
2% Gum Arabic at
4.5pH while
maintaining the
temperature at 40
– 45 0C. The
microcapsules are
rigidized by further
stirring at 20-250C.

100 % pe+ 100 % pe _

Flow diagram of typical phase separation /coacervation
process
 ➢ MULTIORIFIC-CENTRIFUGAL PROCESS:

Coating inlet Material grooves

Coating
material
Core material
inlet
Coating
membrane

Rotating
cylinder
PAN COATING:

o 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.
SPRAY DRYING AND SPRAY CONGEALING

o Spray drying and spray congealing processes are similar in that both
involve dispersing the core material in a liquefied coating substance
and spraying or introducing the core coating mixture into some
environmental condition, whereby, relatively rapid solidification of
the coating is effected.

o The principal difference between the two methods, Coating

solidification in the case of spray drying is effected by rapid
evaporation of a solvent in which the coating material is dissolved.

o Coating solidification in spray congealing method however is

accomplished by thermally congealing a molten coating material or
by solidifying a dissolved coating by introducing the coating core
material mixture into a nonsolvent. Removal of the nonsolvent or
solvent from the coated product is ten accomplished by sorption
extraction or evaporation techniques.
o Microencapsulation by spray drying is conducted by dispersing a
core material in a coating solution, in which the coating substance is
dissolved and in which the core material is insoluble, and then by
atomizing the mixture in to an air stream.

o Micro encapsulation by spray congealing can be accomplished with

spray drying equipment, when the protective coating is applied as
melt.

o Many solidification is accomplished by spraying the hot mixture in to

a cool air stream.

o Waxes, fatty acids, alcohols, polymers & sugars which are solid at
room temperature but meltable at reasonable temperatures, are
applied to spray congealing techniques.
SOLVENT EVAPORATION:

o The process involves dissolving microcapsule coating (polymer) in a

volatile solvent which is immiscible with the liquid manufacturing
vehicle phase. A core material (drug) to be microencapsulated is
dissolved or dispersed in the coating polymer solution.

o With agitation, the core – coating material mixture is dispersed in the

liquid manufacturing vehicle phase to obtain appropriate size
microcapsules. Agitation of system is continued until the solvent
partitions into the aqueous phase and is removed by evaporation.

o Factors that must be considered when preparing microcapsules by

solvent evaporation techniques include choice of vehicle phase and
solvent for the polymer coating, as these choice greatly influence
microcapsule properties as well as the choice of solvent recovery
techniques.
POLYMERIZATION:

o The methods involve the reaction of monomeric units located at the

interface existing between a core material substance and a
continuous phase in which the core material is dispersed.

o Microcapsules having coatings of nylon formed by interfacial

polymerization, or colloidan formed by phase
separation/coacervation techniques.
APPLICATIONS:

The applications of microencapsulation include:

o Sustained release or prolonged action medications.

o Taste masked chewable tablets, powders and suspensions.

o Single layer tablets containing chemically incompatible ingredients

o New formulations concepts for creams, ointments, aerosols,

dressings, plasters, suppositories and injectables.

Physicochemical evaluation characterization:
The physico chemical evaluation include:

❖Morphology Of Microspheres.

❖Particle Size.

❖Density Determination

❖Capture Efficiency.

❖Angle Of Contact.
In Vitro Methods :

❖ 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.

❖ Dissolution Apparatus
– Standard USP or BP dissolution apparatus have been used to
study in vitro release profiles using both rotating elements, paddle
[20, 21, 22 and basket 23, 24].
– Dissolution medium used for the study varied from 100-500 ml and
speed of rotation from 50-100 rpm.