Lec (7) Microencapsulation

Lecture 7
Microencapsulati
on
Dr. Hayder Al-Saadi
Ph.D. Pharmaceuticals
• 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 micro particles,

microcapsules.
•  Particles having diameter between 3 - 800μm are known as micro

particles or microcapsules or microspheres.
 Particles larger than 1000μm are known as Macroparticles.

The applications of microencapsulation include:
1. This technique can be used for converting liquid drugs in a free-flowing powder.
2. The drugs, which are sensitive to oxygen, moisture or light, can be stabilized by
microencapsulation.
3. Incompatibility among the drugs can be prevented by microencapsulation.
4. Vaporization of many volatile drugs e.g. methyl salicylate and peppermint oil can be
prevented by microencapsulation.
5. Many drugs have been microencapsulated to reduce toxicity and GI irritation including
ferrous sulphate and KCl.
6. Alteration in site of absorption can also be achieved by microencapsulation.
7. Controlling the release characteristics or availability of coated materials.
• CLASSIFICATION OF MICROPARTICLE
• Generally Micro particles consist of two components
• a) Core material
• b) Coat or wall or shell material.
• 1.Microcapsules: The active agent forms a core surrounded by an inert diffusion barrier.
• 2.Microspheres: The active agent is dispersed or dissolved in an inert polymer.
• 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.
• Examples of Coating materials:
1. Water soluble resins: Gelatin, Starch, Polyvinylpyrrolidone,
Carboxymethylcellulose, Hydroxyethylcellulose, Methylcellulose,
Arabinogalactan, Polyvinyl alcohol, Polyacrylic acid.

2.Water insoluble resins: Ethylcellulose, Polyethylene,
Polymethacrylate, Polyamide (Nylon), Poly (Ethylene Vinyl acetate),
cellulose nitrate, Silicones, Poly lactideco glycolide.
3.Waxes and lipids: Paraffin, Carnauba, Spermaceti, Beeswax, Stearic

acid, Stearyl alcohol, Glyceryl stearates.
4.Enteric resins: Shellac, Cellulose acetate phthalate, Zein.

• ROLE OF POLYMERS :
 Polymers are substances of high molecular weight made up by repeating

monomer units.
•  Polymer molecules may be linear or branched, and separate linear or

branched chains may be joined by crosslinks.
• Polymers are used widely in pharmaceutical systems as adjuvants, coating

materials and, a components of controlled and site- specific drug delivery
systems
• ADVANTAGES:
• To Increase of bioavailability
• To alter the drug release
• To improve the patient’s compliance
• To produce a targeted drug delivery
• To reduce the reactivity of the core in relation to the outside environment
• To decrease evaporation rate of the core material.
• To convert liquid to solid form & To mask the core taste.
Microencapsulation Methods
1. Air suspension.
2. Coacervation-phase separation.
3. Spray drying and spray congealing.
4. Solvent evaporation techniques.
5. Pan coating.
6. Polymerization techniques.
Air suspension technique
Microencapsulation by air suspension technique consist of the dispersing of solid,
particulate core materials in a supporting air stream and the spray coating 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 parameters effect a recirculating 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.
• During each pass through the coating zone, the core material receives an
increment of coating material.
• The cyclic process is repeated, perhaps several hundred times during processing,
depending on the purpose of microencapsulation, the coating thickness desired,
or whether the core material particles are thoroughly encapsulated.
• The supporting air stream also serves to dry the product while it is being
encapsulated.
• Drying rates are directly related to the volume temperature of the supporting air
stream.
• COACERVATION / PHASE SEPARATION
The processes consists of three steps carried out under continuous agitation:
1. Formation of three immiscible chemical phases.
2. Deposition of the coating.
3. Rigidization of the coating.

Step 1 of the process is the formation of three immiscible phases: a liquid
manufacturing vehicle phase, a core material phase, and a coating material
phase. To form the three phases, the core material is dispersed in a solution of
the coating polymer, the solvent for the polymer being the liquid
manufacturing vehicle phase. The coating material phase, an immiscible
polymer in a liquid state, is formed by utilization of one of the methods of phase
separation-coacervation, that is, by changing the temperature of polymer
solution; or by adding a salt, nonsolvent, or incompatible polymer to the
polymer solution, or by inducing a polymer- polymer interaction
Step 2 of the process consist of depositing of the liquid polymer coating upon
the core material. This is accomplished by controlled, physical mixing of the
coating material (white liquid) and the core material in the manufacturing
vehicle.
Deposition of the liquid polymer coating around the core material occur if the
polymer adsorb at the interface formed between the core material and liquid
vehicle phase, and this adsorption phenomenon is a prerequisite to effective
coating.
Step 3 of the process involve rigidizing the coating, usually by thermal, cross
linking, or de-solvation technique, to form a self-sustaining microcapsules
Spray-drying and spray-congealing
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 (and formation) of the coating is
affected.
• The principal difference between the two methods is the means by which coating solidification is
accomplished.
Coating solidification in the case of spray drying is affected by rapid evaporation of a solvent in
which the coating material is dissolved.
• Coating solidification in spray congealing methods 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 then accomplished by sorption,
extraction, or evaporation techniques.

Spray drying spray = aqueous solution
Spray congealing : spray = hot melt
• The process produces microcapsules approaching a spherical structure in the size range of 5 to 600
microns.
• Characteristically, spray drying yields products of low bulk density, owing to the porous nature of
the coated particles.
• Microencapsulation by spray drying and spray congealing is quite similar, they can be accomplished
with same spray drying equipment and the general process variables and conditions are similar,
except that in spray congealing the core material is dispersed in a coating material melt rather than a
coating solution.
• Coating solidification is accomplished by spraying the hot mixture into a cool air stream.
• Waxes, fatty acids and alcohols, polymers and sugars, which are solids at room temperature but
meltable at reasonable temperatures
Solvent evaporation
The processes are carried out in a liquid manufacturing vehicle.
The microcapsule coating is dissolved in a volatile solvent, which is immiscible

with the liquid manufacturing vehicle phase.
A core material to be microencapsulated is dissolved or dispersed in the coating

polymer solution. With agitation, the core coating material mixture is dispersed
in the liquid manufacturing vehicle phase to obtain the appropriate size
microcapsule.
Solvent evaporation
• The mixture is then heated to evaporate the solvent for the polymer.
• In the case in which the core material is dispersed in the polymer solution,
polymer shrinks around the core.
• In the case in which the core material is dissolved in the coating polymer
solution, a matrix-type microcapsule is formed.
• Once all the solvent for the polymer is evaporated, the liquid vehicle
temperature is reduced to ambient temperature with continued agitation. At
this stage, the microcapsules can be used in suspension form, coated on to
substrates or isolated as powders.
Pan coating
Macro-encapsulation of relatively large particles by pan method has become
widespread in pharmaceutical industry.
The coating applied as a solution, or as automized spray, to the desired solid
core material in the coating pan.
To remove the coating solvent, warmed air is passed over the coated materials
as the coating are being applied in the coating pan.
In some cases, final solvent removal is done in drying oven.

Polymerization
• 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.
• The continuous or core material supporting phase is usually a liquid or gas,

and therefore the polymerization reaction occurs at a liquid-liquid, liquid-gas,
solid-liquid, or solid-gas interface.

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Lecture 7

•  The product obtained by this process is called as micro particles,

•  Particles having diameter between 3 - 800μm are known as micro

 Particles larger than 1000μm are known as Macroparticles.

sorption, solubility, stability, and clarity must be considered in the selection of

the proper microcapsule coating material.

• Examples of Coating materials:

1. Water soluble resins: Gelatin, Starch, Polyvinylpyrrolidone,

Carboxymethylcellulose, Hydroxyethylcellulose, Methylcellulose,

Arabinogalactan, Polyvinyl alcohol, Polyacrylic acid.

3.Waxes and lipids: Paraffin, Carnauba, Spermaceti, Beeswax, Stearic

4.Enteric resins: Shellac, Cellulose acetate phthalate, Zein.

 Polymers are substances of high molecular weight made up by repeating

•  Polymer molecules may be linear or branched, and separate linear or

• Polymers are used widely in pharmaceutical systems as adjuvants, coating

Microencapsulation by air suspension technique consist of the dispersing of solid,

an upward moving air stream.

1. Formation of three immiscible chemical phases.

2. Deposition of the coating.

3. Rigidization of the coating.

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 (and formation) of the coating is

which the coating material is dissolved.

• Coating solidification in spray congealing methods is accomplished by thermally congealing a molten

extraction, or evaporation techniques.

The processes are carried out in a liquid manufacturing vehicle.

The microcapsule coating is dissolved in a volatile solvent, which is immiscible

A core material to be microencapsulated is dissolved or dispersed in the coating

widespread in pharmaceutical industry.

The coating applied as a solution, or as automized spray, to the desired solid

core material in the coating pan.

as the coating are being applied in the coating pan.

In some cases, final solvent removal is done in drying oven.

• The continuous or core material supporting phase is usually a liquid or gas,

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