Microencapsulation
Introduction,
Advantages and
disadvantages,
Methods of
encapsulation
- Snehal Jagtap
Introduction -
Definition : “Microencapsulation
is a process in which active
substances are coated by
extremely small capsules.”
“Microencapsulation is a
process by which solids, liquids
or even gases can be enclosed
in microscopic particles by
formation of thin coating of wall
material (polymer) around the
substance.”
Types -
Microencapsulation [
1 to 800
micrometers]
Microencapsulation [
800 to 1000
micrometers]
Theory of encapsulation-
1) Core material
2) Coating material
Core material (API)
Additives
Preservatives
Diluent
Disintegrents
Preservatives
Stabilizers
Coating material
1) Water soluble resins Ex. Gelatin, gum acacia, starch,
methyl cellulose
2) Water insoluble resins Ex. Ethyl cellulose, silicon
3) Waxes and lipids Ex. Paraben, bees wax, stearic
acid
4) Enteric resins Ex. Shellac, Cellulose acetate
Advantages-
It Masks the taste of bitter drugs to make them more palatable and
improving patient compliance.
Conversion of a liquid dosage form to pseudo solid or free-flowing
powder.
To provide environmental protection of the core material from moisture,
light, and oxygen.
To formulate sustained or prolonged release dosage forms that
continuously release the drugs at a constant rate for a set period.
To alter the physical and surface properties of certain drugs.
Disadvantages -
The cost of the materials used and the formulation process
might be higher than standard formulations.
Unstable release characteristics.
Incomplete or discontinued coating.
Inadequate stability and shelf life.
Methods of microencapsulation -.
• Physicomechanical methods
• Physicochemical methods
• Chemical methods
A] Physicochemical methods
1. Air suspension
2. Centrifugal extrusion
3. Pan coating
4. Spray drying – co-current
- counter current
- mix flow
5. Vibrational nosal method
B] Physicochemical
methods
1. Ionotropic gelatin
2. Coacervation
C] Chemical methods
1. Solvent evaporation
2. Polymerization - interfacial
- in situ
- matrix method
[A] Physicomechanical methods
1]Air suspension coating
• Developed by Prof. Dale E. Wurster.
Factors to be considered…..
1. Properties of drug material and coating material
2. Concentration of coating material
3. Coating material application rate
4. Amount of coating of coating material
5. Inset and outlet pressure operative maintenance
Air suspension
Process-
2] Centrifugal extrusion
• Centrifugal extrusion is a liquid coextrusion process utilizing nozzles consisting. of a
concentric orifice located on the outer circumference of a rotating cylinder. i.e., the head.
• Centrifugal extrusionLiquids 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., up to 22.5 kg of microcapsules can
be produced per nozzle per hour per head.
• Heads containing 16 nozzles are available.
3] Pan coating
• Pan Coating process is used for solid particles greater
than 600 microns in size.
• The coating is applied as a solution, or as an atomized
spray, to the desired solid core material in the coating pan.
4] Spray drying
Process….
Instruments of spray dryer
1. Air heater
2. Automizer (used to reduce molecularsize )
3. Main chamber
4. Cyclon
5. Blender / fan
6. Product collector
Co-current flow
• In a co-current flow spray dryer, the spray is directed into the hot
air entering the dryer and both pass through the chamber in the
same direction
Counter current
• In counter-current spray drying, the material to dry and the air
are injected at opposite location in the drying chamber
Mixed flow
• It combines both co-current
and counter current flow.
5] Vibration nozzel method
• A fluid stream of liquid core and shell material is
pumped through concentric tubes and forms
droplets under the influence of vibration.
• Particle size 100-500 micrometer
• Capacity is 1 - 10,000 kg/ hr
[B] Physicochemical methods
1]Ionotropic gelation
• Ionotropic gelation (IG) is a technique that allows the production of nanoparticles and
microparticles by electrostatic interactions between two ionic species under certain
conditions. At least one of the species has to be a polymer.
• Example ..
Chemical reaction between sodium algenate or barium chloride with
verapamil, reduces the gastric irritation of Verapamil (antihypertensive)
2] Co-acervation
• Coacervation can be defined as the separation of a
macromolecular solution into two immiscible liquid
phases: a dense coacervate phase and a dilute
equilibrium one.
Process-
(a)Core material dispersion in
solution of shell polymer;
(b) separation of coacervate from
solution;
(c) coating of core material by
microdroplets of coacervate;
(d)Coacervance of coacervate to
form continuous shell around
core particles.
[C] Chemical methods
1] Solvent evaporation
In the solvent evaporation method, the drug is dissolved,
dispersed, or emulsified into an organic polymer solution,
which is then emulsified into an external aqueous or oil
phase.
The microspheres are formed after solvent diffusion/evaporation
and polymer precipitation.
2] Polymerization
i) Interfacial
ii) In-situ
iii) Matrix
i) Interfacial polymerization
• Interfacial polymerization is a
type of step-growth
polymerization in which
polymerization occurs at the
interface between two immiscible
phases (generally two liquids),
resulting in a polymer that is
constrained to the interface.
ii) In-situ polymerization
• In some
Polymerization
processes,
direct
Polymerization of
single monomer
is carried out on
the particle
surface.
iii) Matrix Polymerization
•A core material is imbedded in a
polymeric matrix during formation of
particles.

Microencapsulation

  • 1.
  • 2.
    Introduction - Definition :“Microencapsulation is a process in which active substances are coated by extremely small capsules.” “Microencapsulation is a process by which solids, liquids or even gases can be enclosed in microscopic particles by formation of thin coating of wall material (polymer) around the substance.”
  • 3.
    Types - Microencapsulation [ 1to 800 micrometers] Microencapsulation [ 800 to 1000 micrometers]
  • 4.
    Theory of encapsulation- 1)Core material 2) Coating material
  • 5.
  • 6.
    Coating material 1) Watersoluble resins Ex. Gelatin, gum acacia, starch, methyl cellulose 2) Water insoluble resins Ex. Ethyl cellulose, silicon 3) Waxes and lipids Ex. Paraben, bees wax, stearic acid 4) Enteric resins Ex. Shellac, Cellulose acetate
  • 7.
    Advantages- It Masks thetaste of bitter drugs to make them more palatable and improving patient compliance. Conversion of a liquid dosage form to pseudo solid or free-flowing powder. To provide environmental protection of the core material from moisture, light, and oxygen. To formulate sustained or prolonged release dosage forms that continuously release the drugs at a constant rate for a set period. To alter the physical and surface properties of certain drugs.
  • 8.
    Disadvantages - The costof the materials used and the formulation process might be higher than standard formulations. Unstable release characteristics. Incomplete or discontinued coating. Inadequate stability and shelf life.
  • 9.
    Methods of microencapsulation-. • Physicomechanical methods • Physicochemical methods • Chemical methods
  • 10.
    A] Physicochemical methods 1.Air suspension 2. Centrifugal extrusion 3. Pan coating 4. Spray drying – co-current - counter current - mix flow 5. Vibrational nosal method
  • 11.
    B] Physicochemical methods 1. Ionotropicgelatin 2. Coacervation C] Chemical methods 1. Solvent evaporation 2. Polymerization - interfacial - in situ - matrix method
  • 12.
    [A] Physicomechanical methods 1]Airsuspension coating • Developed by Prof. Dale E. Wurster. Factors to be considered….. 1. Properties of drug material and coating material 2. Concentration of coating material 3. Coating material application rate 4. Amount of coating of coating material 5. Inset and outlet pressure operative maintenance
  • 13.
  • 14.
  • 15.
    2] Centrifugal extrusion •Centrifugal extrusion is a liquid coextrusion process utilizing nozzles consisting. of a concentric orifice located on the outer circumference of a rotating cylinder. i.e., the head. • Centrifugal extrusionLiquids 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., up to 22.5 kg of microcapsules can be produced per nozzle per hour per head. • Heads containing 16 nozzles are available.
  • 16.
    3] Pan coating •Pan Coating process is used for solid particles greater than 600 microns in size. • The coating is applied as a solution, or as an atomized spray, to the desired solid core material in the coating pan.
  • 19.
  • 20.
    Instruments of spraydryer 1. Air heater 2. Automizer (used to reduce molecularsize ) 3. Main chamber 4. Cyclon 5. Blender / fan 6. Product collector
  • 21.
    Co-current flow • Ina co-current flow spray dryer, the spray is directed into the hot air entering the dryer and both pass through the chamber in the same direction
  • 22.
    Counter current • Incounter-current spray drying, the material to dry and the air are injected at opposite location in the drying chamber
  • 23.
    Mixed flow • Itcombines both co-current and counter current flow.
  • 24.
    5] Vibration nozzelmethod • A fluid stream of liquid core and shell material is pumped through concentric tubes and forms droplets under the influence of vibration. • Particle size 100-500 micrometer • Capacity is 1 - 10,000 kg/ hr
  • 25.
    [B] Physicochemical methods 1]Ionotropicgelation • Ionotropic gelation (IG) is a technique that allows the production of nanoparticles and microparticles by electrostatic interactions between two ionic species under certain conditions. At least one of the species has to be a polymer. • Example .. Chemical reaction between sodium algenate or barium chloride with verapamil, reduces the gastric irritation of Verapamil (antihypertensive)
  • 26.
    2] Co-acervation • Coacervationcan be defined as the separation of a macromolecular solution into two immiscible liquid phases: a dense coacervate phase and a dilute equilibrium one.
  • 27.
    Process- (a)Core material dispersionin solution of shell polymer; (b) separation of coacervate from solution; (c) coating of core material by microdroplets of coacervate; (d)Coacervance of coacervate to form continuous shell around core particles.
  • 28.
    [C] Chemical methods 1]Solvent evaporation In the solvent evaporation method, the drug is dissolved, dispersed, or emulsified into an organic polymer solution, which is then emulsified into an external aqueous or oil phase. The microspheres are formed after solvent diffusion/evaporation and polymer precipitation.
  • 30.
  • 31.
    i) Interfacial polymerization •Interfacial polymerization is a type of step-growth polymerization in which polymerization occurs at the interface between two immiscible phases (generally two liquids), resulting in a polymer that is constrained to the interface.
  • 32.
    ii) In-situ polymerization •In some Polymerization processes, direct Polymerization of single monomer is carried out on the particle surface.
  • 33.
    iii) Matrix Polymerization •Acore material is imbedded in a polymeric matrix during formation of particles.