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MICROENCAPSULATION TECHNIQUES
INTRODUCTION

 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 .
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.
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.
FUNDAMENTAL CONSIDERATION:

                   Microencapsulation




   Core material        Coating material            Vehicle



Solid     Liquid
                              Polymers          Aqueous   Nonaqueous
                              Waxes

                              Resins
                              Proteins
                              Polysaccharides
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
MICROENCAPSULATION TECHNIQUES:

Air suspension techniques( Wurster)
 Coacervation process
 Spraydrying & congealing
 Pan coating
 Solvent evaporation
 Polymerization
 Extrusion
 Single & double emulsion techniques
 Supercritical fluid anti solvent method (SAS)
 Nozzle vibration technology
WURSTER PROCESS:
COMPLEX COACERVATION :
SOLVENT EVAPORATIONS

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




  Spray drying : spray = aqueous solution / Hot air

  Spray congealing : spray = hot melt/cold air
POLYMERIZATION:

   Drug
            Monomer(s) (e.g. acrylamide, methacrylic acid)           Monodisperse microgels in the micron or
             + Cross-linker (e.g. methylenebisacrylamide)
                                                                     submicron size range.

              Preparation of the
            Polymerization Mixture            Alcohol
                                                                     Precipitation polymerization starts from
                                Addition of the alcoholic solution
                                                                     a homogeneous monomer solution in
                                  of the initiator (e.g., AIBN)      which the synthesized polymer is
                                                                     insoluble.
                Initiation of
               Polymerization
                                                                     The particle size of the resulting
                         8 hrs Reaction time
                                                                     microspheres depends on the
                                                                     polymerization conditions, including the
             Monodisoerse Latex
            Formation by Polymer                                     monomer/co monomer composition, the
                Precipitation
                                                                     amount of initiator and the total
                             T (reaction) = 60 °C
                                                                     monomer concentration.
                            Nitrogen Atmosphere


          RECOVERY OF POLYMERIC
              MICROPARTICLES
EXTRUSION:
•   This method was first patented in 1957.

•   The advantage of extrusion is that it completely surrounds the core
    material with wall material.

•   The process involves forcing a core material dispersed in a molten
    carbohydrate mass through a series of dies, into a bath of dehydrating
    liquid.

•   When contact with the liquid is made, the carbohydrate case hardens to
    entrap the core material.

•   The extruded filaments are separated from the liquid bath, dried using an
    anti-caking agent such as calcium tripolyphosphate and sized .


•   This process is particularly useful for heat labile substances such as
    flavours, vitamin C and colours.
SINGLE EMULSION TECHNIQUE :
DOUBLE EMULSION TECHNIQUES:
NOZZLE VIBRATION TECHNOLOGY :
SAS METHOD :
APPLICATION OF MICROENCAPSULATION TECHNIQUES:
CONCLUSION:

•   The microencapsulation technique offers a variety of opportunities such as
    protection and masking, reduced dissolution rate, facilitation of handling,
    and spatial targeting of the active ingredient.



    This approach facilitates accurate delivery of small quantities of potent
    drugs, reduced drug concentrations at sites other than the target organ or
    tissue and protection of labile compounds before and after administration
    and prior to appearance at the site of action.



•    In future by combining various other approaches,microencapsulation
    technique will find the vital place in novel drug delivery system.
Microencapsulation

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Microencapsulation

  • 2. INTRODUCTION  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 .
  • 3. 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.
  • 4. 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.
  • 5. FUNDAMENTAL CONSIDERATION: Microencapsulation Core material Coating material Vehicle Solid Liquid Polymers Aqueous Nonaqueous Waxes Resins Proteins Polysaccharides
  • 6. 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
  • 7. MICROENCAPSULATION TECHNIQUES: Air suspension techniques( Wurster)  Coacervation process  Spraydrying & congealing  Pan coating  Solvent evaporation  Polymerization  Extrusion  Single & double emulsion techniques  Supercritical fluid anti solvent method (SAS)  Nozzle vibration technology
  • 9.
  • 11. SOLVENT EVAPORATIONS Active Ingredient Polymer + Volatile organic solvent Step 1: Formation of a solution/dispersion of the drug into an organic polymer Organic Polymeric Phase phase. Addition into an aqueous phase (+o/w stabilizer) Step 2: Formation of Oil-in-Water Emulsification of the Emulsion polymer phase into an aqueous phase containing a suitable stabilizer, thus, Temperature increase forming a o/w emulsion. Solvent Evaporation Step 3: Removal of the organic Particle Formation by solvent from the dispersed phase by Polymer Precipitation extraction or evaporation leading to polymer precipitation and formation RECOVERY OF POLYMERIC of the microspheres. MICROPARTICLES
  • 12. SPRAY DRYING & CONGEALING ( COOLING) Spray drying : spray = aqueous solution / Hot air Spray congealing : spray = hot melt/cold air
  • 13. POLYMERIZATION: Drug Monomer(s) (e.g. acrylamide, methacrylic acid) Monodisperse microgels in the micron or + Cross-linker (e.g. methylenebisacrylamide) submicron size range. Preparation of the Polymerization Mixture Alcohol Precipitation polymerization starts from Addition of the alcoholic solution a homogeneous monomer solution in of the initiator (e.g., AIBN) which the synthesized polymer is insoluble. Initiation of Polymerization The particle size of the resulting 8 hrs Reaction time microspheres depends on the polymerization conditions, including the Monodisoerse Latex Formation by Polymer monomer/co monomer composition, the Precipitation amount of initiator and the total T (reaction) = 60 °C monomer concentration. Nitrogen Atmosphere RECOVERY OF POLYMERIC MICROPARTICLES
  • 14. EXTRUSION: • This method was first patented in 1957. • The advantage of extrusion is that it completely surrounds the core material with wall material. • The process involves forcing a core material dispersed in a molten carbohydrate mass through a series of dies, into a bath of dehydrating liquid. • When contact with the liquid is made, the carbohydrate case hardens to entrap the core material. • The extruded filaments are separated from the liquid bath, dried using an anti-caking agent such as calcium tripolyphosphate and sized . • This process is particularly useful for heat labile substances such as flavours, vitamin C and colours.
  • 20. CONCLUSION: • The microencapsulation technique offers a variety of opportunities such as protection and masking, reduced dissolution rate, facilitation of handling, and spatial targeting of the active ingredient. This approach facilitates accurate delivery of small quantities of potent drugs, reduced drug concentrations at sites other than the target organ or tissue and protection of labile compounds before and after administration and prior to appearance at the site of action. • In future by combining various other approaches,microencapsulation technique will find the vital place in novel drug delivery system.