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MICROSPHERES-TYPES ,PREPARATION
,EVALUATION AND APPLICATIONS
PRESENTED BY
SUJITHA MARY
M PHARM
ST JOSEPH COLLEGE OF PHARMACY
1
CONTENTS
INTRODUCTION
CLASSIFICATION OF POLYMERS
METHODS OF PREPARATION
RELEASE FROM MICROSPHERE
MECHANISAM OF
DRUGCHARACTERIZATION
APPLICATIONS
CONCLUSION.
REFERENCES
2
INTRODUCTION
Definition of microspheres
Microparticles or microspheres are defined as small spheres
made of any material and sized from about 50 nm to about 2 mm.
The term nanospheres is often applied to the smaller spheres
(sized 10 to 500 nm) to distinguish them from larger
microspheres.
Microbeads and beads are used alternatively for microsphere
3
Ideally, microspheres are completely spherical and homogeneous
in size.
4
Types of Microspheres
Microcapsule: consisting of an encapsulated core particle. Entrapped
substance completely surrounded by a distinct capsule wall.
Types of Microspheres Microcapsule Micromatrix
Micromatrix: Consisting of homogenous dispersion of active ingredient in
particle
5
Polymers used in the Microsphere preparation
Synthetic polymer
Non-biodegradable
Epoxy polymers
Acrolein
PMMA
Biodegradable
Polyanhydrides
Polyalkyl cyanoacrylates
Lactides and Glycolides copolymers
6
Natural Materials
Proteins
Collagen
Gelatin
Albumins
Carbohydrates
Chitosan
Carrageenan
Starch agarose
Chemically modified carbohydrates
Poly(acryl)starch
Poly(acryl)dextran
7
GENERAL METHODS OF PREPARATION
Single Emulsion techniques
Double emulsion techniques
Polymerization techniques
- Normal polymerization.
- Interfacial polymerization
Coacervation phase separation techniques
Solvent extraction
Spray drying and spray congealing
8
9
10
11
12
Suspension polymerization
13
14
Interfacial Polymerization
technique
When two reactive monomers are dissolved in immiscible
solvents, the monomers diffuse to the oil- water interface where
they react to form a polymeric membrane that envelopes
dispersed phase.
Drug is incorporated either by being dissolved in the
polymerization medium or by adsorption onto the nanoparticles
after polymerization completed.
The nanoparticle suspension is then purified to remove various
stabilizers and surfactants employed for polymerization by
ultracentrifugation and resuspending the particles in an isotonic
surfactant-free medium.
15
16
PHASE SEPARATION
METHOD
17
Salting-out process
An aqueous phase saturated with electrolytes (e.g., magnesium
acetate, magnesium chloride) and containing PVA as a stabilizing
and viscosity increasing agent is added under vigorous stirring to
an acetone solution of polymer.
In this system, the miscibility of both phases is prevented by the
saturation of the aqueous phase with electrolytes, according to a
salting-out phenomenon.
The addition of the aqueous phase is continued until a phase
inversion occurs and an o/w emulsion is formed
18
19
Emulsification-Solvent
evaporation method
20
DRUG LOADING
During the preparation of microspheres or after the formation of
microspheres by incubating.
Loading into preformed microspheres has an advantage of
removing all impurities from microsphere preparation before the
drug is incorporated
High loading can be achieved by insitu loading.
If the drug is insoluble in dispersion medium employed for
microsphere stabilization.
21
ROUTE OF
ADMINISTRATION
ORAL DELIVERY
PARENTERAL DELIVERY
22
MECHANISM OF DRUG RELEASE
Degradation controlled monolithic system.
Diffusion controlled monolithic system
Diffusion controlled reservoir system.
Erodable polyagent system.
23
Characterisation
24
PARTICLE SIZE
25
CAPTURE EFFICIENCY
26
POTENTIAL USE OF MICROSPHERESIN THE
PHARMACEUTICAL INDUSTRY
Taste and odour masking.
Conversion of oils and other liquids to solids for ease of handling
Protection of drugs against the environment (moisture, light etc.).
Separation of incompatible materials (other drugs or excipients).
Improvement of flow of powders
Aid in dispersion of water-insoluble substances in aqueous
media, and Production of SR, CR, and targeted medications.
27
OTHER APPLICATIONS
 Microcapsules are also extensively used as diagnostics, for example,
temperature-sensitive microcapsules for thermographic detection of tumors.
In the biotechnology industry microencapsulated microbial cells are being
used for the production of recombinant proteins and peptides.
Encapsulation of microbial cells can also increase the cell- loading capacity
and the rate of production in bioreactors.
A feline breast tumor line, which was difficult to grow in conventional culture,
has been successfully grown in microcapsules.
Microencapsulated activated charcoal has been used for hemoperfusion.
28
These Microspheres are free-flowing and roll with practically no
friction, that means there is no abrasion, guaranteeing a dust-free
environment.
These carriers received much attention not only for prolonged
release but also for the targeting anti cancer drugs to the tumour.
Solid biodegradable microspheres incorporating a drug
dispersed or dissolved throughout particle matrix have the
potential for controlled release of the drug.
Microspheres are made from polymeric , waxy or protective
materials that is biodegradable synthetic polymers and modified
natural products.
29
MARKETED PRODUCTS
30
CONCLUSION
The concept of microsphere drug delivery systems offers certain
advantages over the conventional drug delivery systems such as
controlled and sustained delivery. Apart from that microspheres
also allow drug targeting to various systems such as ocular ,
intranasal , oral and IV route
Novel technologies like magnetic microspheres,
immunomicrospheres offer great advantages and uses than
conventional technologies.
31
Further more in future by combining various other strategies,
microspheres will find the central place in novel drug delivery,
particularly in diseased cellsorting ,diagnostics, gene and genetic
materials, safe,targated and effective invivo delivery which may
have implications in gene therapy.
This area of novel drug delivery has innumerable applications
and there is a need for more research to be done in this area.
32
REFERENCES
Controlled Drug Delivery Novel Carrier Systems., S.P.Vyas.,
R.K.Khar, First Edition :2002.,Reprint :2007 page no:417,453.
Review: Radioactive Microspheres for Medical Applications.
International journal of Pharmaceutics 282 (2004) 1- 18,Review
polymer microspheres for controlled drug release.
Controlled and novel drug delivery edited by N.K.Jain reprint 2007
pg.no.236-255
International Journal for Targeted&
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2811640
33
34
35

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Microspheres types preparation evaluation and application

  • 1. MICROSPHERES-TYPES ,PREPARATION ,EVALUATION AND APPLICATIONS PRESENTED BY SUJITHA MARY M PHARM ST JOSEPH COLLEGE OF PHARMACY 1
  • 2. CONTENTS INTRODUCTION CLASSIFICATION OF POLYMERS METHODS OF PREPARATION RELEASE FROM MICROSPHERE MECHANISAM OF DRUGCHARACTERIZATION APPLICATIONS CONCLUSION. REFERENCES 2
  • 3. INTRODUCTION Definition of microspheres Microparticles or microspheres are defined as small spheres made of any material and sized from about 50 nm to about 2 mm. The term nanospheres is often applied to the smaller spheres (sized 10 to 500 nm) to distinguish them from larger microspheres. Microbeads and beads are used alternatively for microsphere 3
  • 4. Ideally, microspheres are completely spherical and homogeneous in size. 4
  • 5. Types of Microspheres Microcapsule: consisting of an encapsulated core particle. Entrapped substance completely surrounded by a distinct capsule wall. Types of Microspheres Microcapsule Micromatrix Micromatrix: Consisting of homogenous dispersion of active ingredient in particle 5
  • 6. Polymers used in the Microsphere preparation Synthetic polymer Non-biodegradable Epoxy polymers Acrolein PMMA Biodegradable Polyanhydrides Polyalkyl cyanoacrylates Lactides and Glycolides copolymers 6
  • 8. GENERAL METHODS OF PREPARATION Single Emulsion techniques Double emulsion techniques Polymerization techniques - Normal polymerization. - Interfacial polymerization Coacervation phase separation techniques Solvent extraction Spray drying and spray congealing 8
  • 9. 9
  • 10. 10
  • 11. 11
  • 12. 12
  • 14. 14
  • 15. Interfacial Polymerization technique When two reactive monomers are dissolved in immiscible solvents, the monomers diffuse to the oil- water interface where they react to form a polymeric membrane that envelopes dispersed phase. Drug is incorporated either by being dissolved in the polymerization medium or by adsorption onto the nanoparticles after polymerization completed. The nanoparticle suspension is then purified to remove various stabilizers and surfactants employed for polymerization by ultracentrifugation and resuspending the particles in an isotonic surfactant-free medium. 15
  • 16. 16
  • 18. Salting-out process An aqueous phase saturated with electrolytes (e.g., magnesium acetate, magnesium chloride) and containing PVA as a stabilizing and viscosity increasing agent is added under vigorous stirring to an acetone solution of polymer. In this system, the miscibility of both phases is prevented by the saturation of the aqueous phase with electrolytes, according to a salting-out phenomenon. The addition of the aqueous phase is continued until a phase inversion occurs and an o/w emulsion is formed 18
  • 19. 19
  • 21. DRUG LOADING During the preparation of microspheres or after the formation of microspheres by incubating. Loading into preformed microspheres has an advantage of removing all impurities from microsphere preparation before the drug is incorporated High loading can be achieved by insitu loading. If the drug is insoluble in dispersion medium employed for microsphere stabilization. 21
  • 23. MECHANISM OF DRUG RELEASE Degradation controlled monolithic system. Diffusion controlled monolithic system Diffusion controlled reservoir system. Erodable polyagent system. 23
  • 27. POTENTIAL USE OF MICROSPHERESIN THE PHARMACEUTICAL INDUSTRY Taste and odour masking. Conversion of oils and other liquids to solids for ease of handling Protection of drugs against the environment (moisture, light etc.). Separation of incompatible materials (other drugs or excipients). Improvement of flow of powders Aid in dispersion of water-insoluble substances in aqueous media, and Production of SR, CR, and targeted medications. 27
  • 28. OTHER APPLICATIONS  Microcapsules are also extensively used as diagnostics, for example, temperature-sensitive microcapsules for thermographic detection of tumors. In the biotechnology industry microencapsulated microbial cells are being used for the production of recombinant proteins and peptides. Encapsulation of microbial cells can also increase the cell- loading capacity and the rate of production in bioreactors. A feline breast tumor line, which was difficult to grow in conventional culture, has been successfully grown in microcapsules. Microencapsulated activated charcoal has been used for hemoperfusion. 28
  • 29. These Microspheres are free-flowing and roll with practically no friction, that means there is no abrasion, guaranteeing a dust-free environment. These carriers received much attention not only for prolonged release but also for the targeting anti cancer drugs to the tumour. Solid biodegradable microspheres incorporating a drug dispersed or dissolved throughout particle matrix have the potential for controlled release of the drug. Microspheres are made from polymeric , waxy or protective materials that is biodegradable synthetic polymers and modified natural products. 29
  • 31. CONCLUSION The concept of microsphere drug delivery systems offers certain advantages over the conventional drug delivery systems such as controlled and sustained delivery. Apart from that microspheres also allow drug targeting to various systems such as ocular , intranasal , oral and IV route Novel technologies like magnetic microspheres, immunomicrospheres offer great advantages and uses than conventional technologies. 31
  • 32. Further more in future by combining various other strategies, microspheres will find the central place in novel drug delivery, particularly in diseased cellsorting ,diagnostics, gene and genetic materials, safe,targated and effective invivo delivery which may have implications in gene therapy. This area of novel drug delivery has innumerable applications and there is a need for more research to be done in this area. 32
  • 33. REFERENCES Controlled Drug Delivery Novel Carrier Systems., S.P.Vyas., R.K.Khar, First Edition :2002.,Reprint :2007 page no:417,453. Review: Radioactive Microspheres for Medical Applications. International journal of Pharmaceutics 282 (2004) 1- 18,Review polymer microspheres for controlled drug release. Controlled and novel drug delivery edited by N.K.Jain reprint 2007 pg.no.236-255 International Journal for Targeted& http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2811640 33
  • 34. 34
  • 35. 35