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By SARADA ANEPU

 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.

Particles having diameter between 3 - 800µm are known as micro particles or microcapsules or microspheres.

Particles larger than 1000µm are known as Macroparticles .

 To mask the bitter taste of drugs
 To reduce gastric irritations  A liquid can be converted to a pseudo-solid for easy handling and storage  Hygroscopic properties of core materials may be reduced by

microencapsulation
 To reduce their odor and volatility.  Protection to the core materials against atmospheric effects  Separation of incompatible substance

Microcapsules: The active agent forms a core surrounded by an inert diffusion barrier.Microspheres: The active agent is dispersed or dissolved in an inert polymer . Microcapsules have well defined core and well defined envelope 2.Generally Micro particles consist of two components a) Core material b) Coat or wall or shell material 1.

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shear or abrasive force Permeability change brought about by enzymatic fluid  The wall melts away from the core releasing the core in an environment such as that occurring during baking  The core diffuses through the wall at a slow rate due to the influence of an exterior fluid such as water or by an elevated temperature Rate of release depends on Permeability of coating material to extraction fluid Dissolution rate of core Coating thickness Concentration across the membranes .RELEASE MECHANISMS Disruption of the coating by pressure.

o The material to be coated o It may be liquid or solid or gas. o Liquid core may be dissolved or dispersed material COMPOSITION OF CORE MATERIAL: o Drug or active constituent o Additive like diluents o Stabilizers o Release rate enhancers or retardants .

flexibility& impermeability COMPOSITION OF COATING o Inert polymer o Plasticizer o Coloring agent . non reactive & cheap o Provide desired coating properties like strength.Inert substance which coats on core with desired thickness IDEAL CHARACTERISTICS: o Capable of forming a film cohesive with core material o Chemically compatible with the core material o Should be stable.

Synthetic Non biodegradable Acrolein Epoxy polymers Natural Proteins Albumin Gelatin collagen Carbohydrates Biodegradable Polyesters Poly ortho esters Poly anhydrides Polyphosphazenes Starch Agarose Carragreen Chitosan .

Physical Physico chemical • Coacervation • Single emulsion • Double emulsion • RESS method • SAS method Chemical • Solvent Evaporation • Interfacial polymerisation • Matrix Polymerisation • Pan Coating • Fluidized bed • Multi orificecentrifugal process • Spinning disc • Spray drying .

 Pan Coating  Air suspension  Centrifugal extrusion  Spinning disc  Spray drying .

 Preparation of core  Coating procedure .Two steps.

Air suspension process:  .

developed by the Southwest Research Institute as a mechanical process for producing micro-capsules that utilizes centrifugal forces to hurl a core material particle trough an enveloping microencapsulation membrane thereby affecting mechanical microencapsulation.  The encapsulated product can be supplied as slurry in the hardening media . by applying the different coating materials. the flow rate of the coating and core materials and the concentration. Multiorifice-centrifugal process.  The factors that affect process include the rotational speed of the cylinder. viscosity and surface tension of the core material.  This process is capable of producing the microencapsulation of the liquids and solids of varied size ranges.

 Droplets of pure shell material are thrown off of the rim of the disk along with discrete particles of core material enclosed in a skin of shell material. the microcapsules are collected separately from the particles of shell material . In rotational suspension separation.  After having been solidified by cooling. or the spinning disk method internal phase is dispersed into the liquid wall material and the mixture is advanced onto a turning disk.

 The resultant emulsion is atomized into a spray of droplets by pumping the slurry through a rotating disc into the heated compartment of a spray drier. immiscible with water. An emulsion is prepared by dispersing the core material.  The capsules are collected through continuous discharge from the spray drying chamber .  There the water portion of the emulsion is evaporated. into a concentrated solution of wall material until the desired size of oil droplets are attained. yielding dried capsules of variable shape containing scattered drops of core material.

 Coacervation  Single emulsion  Double emulsion  RESS method  SAS method .

Rigidization of coating.Formation of three immiscible phases 2.PHASE SEPARATION Homogeneous Polymer Solution Droplets Coacervate Droplets MEMBRANE FORMATION Polymeric Membrane 1.Deposition of coating 3. .

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Deposition of coating  This step consits of Rigidization of coating Rigidisation of coating occurs by  thermal cross linking or  desolvation technique depositing liqud polymer on core  Deposition ocuurs on the interface which is promoted by decrease in interfacial energy .

 Natural polymers are dissolved in aqueous medium followed by dispersion in aqueous non aqueous medium  For dispersion cross linking is carried out by heat or chemical agents .

Solution of poly vinyl alcohol added  At reduced pressure solvent is removed . water soluble drugs  Primary emulsion prepared subjected to homogenisation  Aq. Involves preperation of multiple emulsions.

. Pressurized supercritical solvent containing the shell material and the active ingredient is released through a small nozzle  The abrupt pressure drop causes the desolvation of the shell material and the formation of a coating layer around the active ingredient.

 On the other hand. . This process is also called supercritical fluid anti-solvent (SAS) method.  Thus.  This leads to a volume expansion of the solution that causes super saturation such that precipitation of the solute occurs. the liquid solvent must be miscible with the supercritical fluid. but should not dissolve in the mixture of solvent and supercritical fluid. Where supercritical fluid is added to a solution of shell material and the active ingredients and maintained at high pressure. the solute must be soluble in the liquid solvent.

 Solvent Evaporation  Interfacial polymerization  Matrix Polymerization .

Step 3: Removal of the organic solvent from the dispersed phase by extraction or evaporation leading to polymer precipitation and formation of the microspheres. thus. forming a o/w emulsion.SOLVENT EVAPORATIONS Active Ingredient Polymer + Volatile organic solvent Organic Polymeric Phase Addition into an aqueous phase (+o/w stabilizer) Formation of Oil-in-Water Emulsion Temperature increase Solvent Evaporation Particle Formation by Polymer Precipitation Step 1: Formation of a solution/dispersion of the drug into an organic polymer phase. RECOVERY OF POLYMERIC MICROPARTICLES . Step 2: Emulsification of the polymer phase into an aqueous phase containing a suitable stabilizer.

. AIBN) Initiation of Polymerization 8 hrs Reaction time Monodisperse Latex Formation by Polymer Precipitation T (reaction) = 60 °C Nitrogen Atmosphere units  Drug is dispersed in the polymeristion mixture  Alcoholic solution is used as initiator  Polymers precipitate  Microparticles recovered RECOVERY OF POLYMERIC MICROPARTICLES .g.g. methylenebisacrylamide)  Reaction of monomeric Preparation of the Polymerization Mixture Alcohol Addition of the alcoholic solution of the initiator (e. acrylamide.g.Drug Monomer(s) (e. methacrylic acid) + Cross-linker (e.

 Proceeds with reaction of monomers at the interface between two immisible liqud phases to form a film of polymer which envelops dispersed phase  One monomer is dissolved and other is dispersed  Continuous phase is usually aqueous in which 2nd monomer is emulsified  Monomers at either phase diffuse rapidly and polymerise at interface of core particles .

 The solidification of the matrix also can be caused by a chemical change. a core material is imbedded in a polymeric matrix during formation of the particles. .  A simple method of this type is spray-drying. In a number of processes. in which the particle is formed by evaporation of the solvent from the matrix material.

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nitrogen .Process Interfacial polymerisation Coating material Water-soluble and insoluble monomers Water-soluble polyelectrolyte Hydrophobic polymers Suspended medium Aqueous/organic solvent Complex coacervation Coacervation Water Organic solvent Solvent evaporation Hydrophilic or hydrophobic polymers Hydrophilic or hydrophobic polymers Organic or water Spray drying Air.

 Stability testing  Size of microcapsules.In vitro drug release .Sieving Method  Amount of drug present In microcapsules  Viscosity of polymer solutions  Dissolution test.

60 and 80 mesh) are arranged in the order of decreasing aperture sizere shaken for a period of about 10 min. and then the particles on the screen are weighed . 30. Separation of the microspheres into various size fractions can be determined by using a mechanical sieve shaker  The sieves (20. 45.

. The surface morphologies of microspheres are examined by a scanning electron microscope  Nature of the microspere is examined  The microspheres are mounted onto a copper Cylinder by using a double-sided adhesive tape.

 Bulk density tapped density are determined  The Hausner ratio of the microcapsules is determined by the following relationship  hr = ρ tapped/ρ bulk  Where ρ tapped is tapped density  ρ bulk is bulk density. .

kinematic viscosity. and the intrinsic viscosity of the polymer solutions in different solvents can be measured by a U-tube viscometer  The polymer solutions are allowed to stand for 24 h prior to measurement to ensure complete polymer dissolution . The absolute viscosity.

 Standard USP or BP dissolution apparatus are used to study in vitro release profiles  Dissolution medium used for the study varied from 100-500 ml and speed of rotation from 50-100 rpm.  Dissolution medium is decided from the drug being encapsulated .

dicumarol  DNA vaccines with prolonged immuno responses . Targeted drug delivery to Peyer’s patch  Live cell encapsulation  Bioadhesive microparticles show enhanced oral bio availability of insulin.

The Theory and Practice of IndustrialPharmacy  S.K.Vyas and R.C. Targeted andControlled drug delivery . Pharmaceutical dosage form and drug delivery system..Josep. Ansel.P.  Lehman Leon. Herbert and KanigL. Lieberman A.H.Khar.