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SHRI R D BHAKT COLLEGE OF PHARAMACY
JALNA, MAHARASHTRA
1
Presented By, Under guidance of,
Miss. Amruta Jain Mr. Sandip Phoke
1. Introduction
2. Literature Review
3. Need And Rationals
4. Method of Preparation
5. Evaluation of Microparticles
6. Summary And conclusion
7. Future Scope
8. References
2
• Definition:
“Microparticles are defined as particulate dispersions
or solid particles with a size in the range of 1-1000 μm.”
• The drug is dissolved, entrapped, encapsulated or attached to
a microparticle matrix.
• Depending upon the method of preparation, microparticles,
microspheres or microcapsules can be obtained.
3
Figure Microparticles
4
 Microencapsulation is a technology used to entrap solids,
liquids, or gases inside a polymeric matrix or shell.
 Two general micro morphologies of microparticles can be
distinguished- microcapsules and microspheres.
Figure: Microcapsules
• Morphology of Microparticle
Figure: Microsphere
5
• Advantages of MPs:
 Taste and odour masking. E.g. Fish oils, sulfa drugs.
 Protection of drugs from environment.
 Particle size reduction for enhancing solubility of the
poorly soluble drug.
 Sustained or controlled drug delivery Eg: KCl, Ibuprofen.
 Targeted release of encapsulated material.
 Live cell encapsulation. Eg: Resealed erythrocytes.
 Aid in dispersion of water insoluble substance in aqueous
media.
6
 The costs of the materials and processing of the controlled
release preparation, which may be substantially higher
than those of standard formulations.
 Reproducibility is less.
 Process conditions like change in temperature, pH, solvent
addition, and evaporation/ agitation may influence the
stability of core particles to be encapsulated.
 The environmental impact of the degradation products of
the polymer matrix produced in response to heat,
hydrolysis, oxidation, solar radiation or biological agents.
• Disadvantages of MPs:
7
• APPLICATIONS OF MPs:
1. Sustained drug delivery
2. Controlled drug delivery
3. Local drug delivery
4. Pulsatile drug delivery
5. Targeted drug delivery
8
9
Author Title Journal
Lu, Z. et al.
(2016)
Tumor-penetrating microparticles for
intraperitoneal therapy of ovarian cancer
Journal of Pharmacology
and Experimental
Therapeutics,
Naikwade, S.
R. et al.
(2016)
Development of budesonide microparticles
using spray-drying technology for
pulmonary administration: design,
characterization, in vitro evaluation, and in
vivo efficacy study.
AAPS PharmSciTech,
Vijaya R. et
al., (2015)
Development of microparticles for
controlled release of antibiotic drug
Ciprofloxacin
World journal of pharmacy
and pharmaceutical sciences
Dalmoro A. et
al. (2015)
Enteric micro-particles for targeted oral
drug delivery.
AAPS PharmSciTech,
YeM. et
al.(2014)
Biodegradable microparticles For long-
term protein delivery
Indian journal of
pharmaceutical and
biological research
10
• Microparticles for capillary electrochromatography studies
on microparticles synthesis and electrolyte composition.
• Microparticles from circulating and vascular cells in
regulating vascular function.
• The use of biodegradable microparticles and nanoparticles
in controlled drug delivery.
• Controlled release of microparticles for vaccine
development.
• Techniques of microparticle preparation
• Emulsion–solvent evaporation (o/w, w/o, w/o/w).
• Phase separation (nonsolvent addition and solvent
partitioning).
• Interfacial polymerization.
• Spray drying.
• Emulsion extraction process.
• Jet milling technique.
• Fluidization & solvent precipitation method.
11
• Techniques of microparticle preparation
• Emulsion–solvent evaporation (o/w, w/o, w/o/w).
• Phase separation (nonsolvent addition and solvent
partitioning).
• Interfacial polymerization.
• Spray drying.
• Emulsion extraction process.
• Jet milling technique.
• Fluidization & solvent precipitation method.
1
2
1
3
• Emulsion-solvent evaporation:
1
4
- The process consists of decreasing the solubility of the
encapsulating polymer by addition of a third component to the
polymer solution .
- The process yields two liquid phases: the polymer containing
coacervate phase and the supernatant phase depleted in
polymer.
- Thus the coacervation process consists of the following three
steps:
i) Phase separation of the coating polymer solution,
ii) Adsorption of the coacervate around the drug
particles,
iii) Solidification of the microspheres.
• Phase Separation::
1
5
- Spray-drying is a widely used method for formulating
biodegradable microparticles.
- It is rapid, convenient, easy to scale-up, involves mild
conditions, and is less dependent on the solubility parameters
of the drug and the polymer.
- The method typically uses drug dissolved or suspended in a
polymer solution (either organic or aqueous solvent depending
on the polymer used).
• Spray drying:
1
6
• Spray drying::
1
7
1. Micromeritics
i. Particle size
ii. Bulk density
iii. Tapped density
iv. Carr’s index (%)
v. Angle of repose (θ)
vi. Hausner’s ratio
vii. Percentage yield
2. Drug entrapment efficiency (DEE)
3. In vitro Buoyancy
4. Dissolution test (in vitro-drug release) of Microballoons
5. Morphological Study using SEM
6. Stability Studies
7. Release kinetics
1
8
-The microparticles drug delivery system is a physical approach
to alter and improve the pharmacokinetic and pharmacodynamics
properties of various types of drug molecules.
-The microparticles offers a variety of opportunities such as
protection and masking, better process ability, improve
bioavailability, decreasing dosing frequency, improve stability,
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.
1
9
• As the primary and more promising fields, microparticles are
utilized in composites, paints and coatings, oil and gas
exploration, adhesives, cosmetics and personal grooming
products, life sciences and biotechnology, medicine and
medical devices.
• Nevertheless, microparticles are still an area of ongoing
research efforts, and outstanding work continues to be
produced by researchers in this field.
• One useful discovery made from the research of microspheres
is a way to fight cancer on a molecular level.
2
0
•Pavan Kumar, B., Sarath Chandiran, I., Bhavya, B., & Sindhuri, M. (2011).
Microparticulate drug delivery system: a review. Indian J Pharm Sci Res, 1(1), 19-37.
• Sharma, P. (2016). Microparticles drug delivery system: a review. World J Pharm
and Pharma Sci. 5(3), 543-566.
•Madhav, N. S., & Kala, S. (2011). Review on microparticulate drug delivery system.
Int J PharmTech Res, 3, 1242-54.
•Gattani, Y. S. (2010). Floating Multiparticulate drug delivery systems: an overview.
International Journal of Pharma and Bio Sciences, 1(2), 1-14.
•Dubey, R. (2009). Microencapsulation technology and applications. Defence Science
Journal, 59(1), 82.
•James Swar Brick, James E. Boylan, Mercel dekkar. Microencapsulation technology
and applications. Encyclopedia of pharmaceutical Technology,10, 1988, 245-286.
•Krishna, R. S. M., Shivakumar, H. G., Gowda, D. V., & Banerjee, S. (2006).
Nanoparticles-a novel colloidal drug delivery system. Indian Journal of
Pharmaceutical Education and Research, 40(1), 15.
•Tuncer Degim, I., & Çelebi, N. (2007). Controlled delivery of peptides and proteins.
Current pharmaceutical design, 13(1), 99-117.
•Alagusundaram, M., Chetty, M. S., Umashankari, K., Badarinath, A. V., Lavanya, C.,
& Ramkanth, S. (2009). Microspheres as a novel drug delivery system-a review. Int J
Chem Tech Res, 1(3), 526-34.
.
2
1
•Sah, H. K., Toddywala, R., & Chien, Y. W. (1995). Biodegradable microcapsules
prepared by aw/o/w technique: effects of shear force to make a primary w/o emulsion
on their morphology and protein release. Journal of microencapsulation, 12(1), 59-69.
•Goto, S., Moriya, F., Kawata, M., & Kimura, T. (1984). Preparation and
biopharmaceutical evaluation of microcapsules of amoxicillin. Journal of
microencapsulation, 1(2), 137-155.
•Kristl, A., Bogataj, M., Mrhar, A., & Kozjek, F. (1991). Preparation and evaluation of
ethylcellulose microcapsules with bacampicillin. Drug development and industrial
pharmacy, 17(8), 1109-1130.
•Hoyer, H., Schlocker, W., Krum, K., & Bernkop-Schnürch, A. (2008). Preparation
and evaluation of microparticles from thiolated polymers via air jet milling. European
Journal of Pharmaceutics and Biopharmaceutics, 69(2), 476-485.
•Lu, Z., Tsai, M., Lu, D., Wang, J., Wientjes, M. G., & Au, J. L. S. (2008). Tumor-
penetrating microparticles for intraperitoneal therapy of ovarian cancer. Journal of
Pharmacology and Experimental Therapeutics, 327(3), 673-682.
•Naikwade, S. R., Bajaj, A. N., Gurav, P., Gatne, M. M., & Soni, P. S. (2009).
Development of budesonide microparticles using spray-drying technology for
pulmonary administration: design, characterization, in vitro evaluation, and in vivo
efficacy study. AAPS PharmSciTech, 10(3), 993-1012.
.
2
2
•Parida, K. R., Panda, S. K., Ravanan, P., Roy, H., Manickam, M., & Talwar, P. (2013).
Microparticles based drug delivery systems: preparation and application in cancer
therapeutics. Cellulose, 17, 18.
•Onishi, H., & Machida, Y. (2008). In vitro and in vivo evaluation of microparticulate
drug delivery systems composed of macromolecular prodrugs. Molecules, 13(9), 2136-
2155.
•Sahil, K., Akanksha, M., Premjeet, S., Bilandi, A., & Kapoor, B. (2011). Microsphere:
A review. Int. J. Res. Pharm. Chem, 1(4), 1184-98.
•Padalkar, A. N., Shahi, S. R., & Thube, M. W. (2011). Microparticles: an approach for
betterment of drug delivery system. Int J Pharm Res Dev, 1, 99-115.
•Kumar, M. N. V. R. (2000). Nano and microparticles as controlled drug delivery
devices. J. Pharm. Pharm. Sci, 3(2), 234-258.
•http://www.omicsonline.org/open-access/microparticles-a-novel-approach-to-
enhance-drug-bioavailability-jbb-10000e68.php?aid=56334#PDF. (accessed on
24/10/2016)
•https://www.tri.edu.au/trans-dermal-drug-delivery-using-elongated-microparticles.
(accessed on 05/11/2016)
•http://www.sciencedirect.com/science/jrnlallbooks/all/open-access. (accessed on 28-
10-2016)
•https://www.ncbi.nlm.nih.gov/pubmed . (accessed on 28-10-2016)
2
3

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Microparticle Drug Delivery System: A Review

  • 1. SHRI R D BHAKT COLLEGE OF PHARAMACY JALNA, MAHARASHTRA 1 Presented By, Under guidance of, Miss. Amruta Jain Mr. Sandip Phoke
  • 2. 1. Introduction 2. Literature Review 3. Need And Rationals 4. Method of Preparation 5. Evaluation of Microparticles 6. Summary And conclusion 7. Future Scope 8. References 2
  • 3. • Definition: “Microparticles are defined as particulate dispersions or solid particles with a size in the range of 1-1000 μm.” • The drug is dissolved, entrapped, encapsulated or attached to a microparticle matrix. • Depending upon the method of preparation, microparticles, microspheres or microcapsules can be obtained. 3
  • 5.  Microencapsulation is a technology used to entrap solids, liquids, or gases inside a polymeric matrix or shell.  Two general micro morphologies of microparticles can be distinguished- microcapsules and microspheres. Figure: Microcapsules • Morphology of Microparticle Figure: Microsphere 5
  • 6. • Advantages of MPs:  Taste and odour masking. E.g. Fish oils, sulfa drugs.  Protection of drugs from environment.  Particle size reduction for enhancing solubility of the poorly soluble drug.  Sustained or controlled drug delivery Eg: KCl, Ibuprofen.  Targeted release of encapsulated material.  Live cell encapsulation. Eg: Resealed erythrocytes.  Aid in dispersion of water insoluble substance in aqueous media. 6
  • 7.  The costs of the materials and processing of the controlled release preparation, which may be substantially higher than those of standard formulations.  Reproducibility is less.  Process conditions like change in temperature, pH, solvent addition, and evaporation/ agitation may influence the stability of core particles to be encapsulated.  The environmental impact of the degradation products of the polymer matrix produced in response to heat, hydrolysis, oxidation, solar radiation or biological agents. • Disadvantages of MPs: 7
  • 8. • APPLICATIONS OF MPs: 1. Sustained drug delivery 2. Controlled drug delivery 3. Local drug delivery 4. Pulsatile drug delivery 5. Targeted drug delivery 8
  • 9. 9 Author Title Journal Lu, Z. et al. (2016) Tumor-penetrating microparticles for intraperitoneal therapy of ovarian cancer Journal of Pharmacology and Experimental Therapeutics, Naikwade, S. R. et al. (2016) Development of budesonide microparticles using spray-drying technology for pulmonary administration: design, characterization, in vitro evaluation, and in vivo efficacy study. AAPS PharmSciTech, Vijaya R. et al., (2015) Development of microparticles for controlled release of antibiotic drug Ciprofloxacin World journal of pharmacy and pharmaceutical sciences Dalmoro A. et al. (2015) Enteric micro-particles for targeted oral drug delivery. AAPS PharmSciTech, YeM. et al.(2014) Biodegradable microparticles For long- term protein delivery Indian journal of pharmaceutical and biological research
  • 10. 10 • Microparticles for capillary electrochromatography studies on microparticles synthesis and electrolyte composition. • Microparticles from circulating and vascular cells in regulating vascular function. • The use of biodegradable microparticles and nanoparticles in controlled drug delivery. • Controlled release of microparticles for vaccine development.
  • 11. • Techniques of microparticle preparation • Emulsion–solvent evaporation (o/w, w/o, w/o/w). • Phase separation (nonsolvent addition and solvent partitioning). • Interfacial polymerization. • Spray drying. • Emulsion extraction process. • Jet milling technique. • Fluidization & solvent precipitation method. 11
  • 12. • Techniques of microparticle preparation • Emulsion–solvent evaporation (o/w, w/o, w/o/w). • Phase separation (nonsolvent addition and solvent partitioning). • Interfacial polymerization. • Spray drying. • Emulsion extraction process. • Jet milling technique. • Fluidization & solvent precipitation method. 1 2
  • 14. 1 4 - The process consists of decreasing the solubility of the encapsulating polymer by addition of a third component to the polymer solution . - The process yields two liquid phases: the polymer containing coacervate phase and the supernatant phase depleted in polymer. - Thus the coacervation process consists of the following three steps: i) Phase separation of the coating polymer solution, ii) Adsorption of the coacervate around the drug particles, iii) Solidification of the microspheres. • Phase Separation::
  • 15. 1 5 - Spray-drying is a widely used method for formulating biodegradable microparticles. - It is rapid, convenient, easy to scale-up, involves mild conditions, and is less dependent on the solubility parameters of the drug and the polymer. - The method typically uses drug dissolved or suspended in a polymer solution (either organic or aqueous solvent depending on the polymer used). • Spray drying:
  • 17. 1 7 1. Micromeritics i. Particle size ii. Bulk density iii. Tapped density iv. Carr’s index (%) v. Angle of repose (θ) vi. Hausner’s ratio vii. Percentage yield 2. Drug entrapment efficiency (DEE) 3. In vitro Buoyancy 4. Dissolution test (in vitro-drug release) of Microballoons 5. Morphological Study using SEM 6. Stability Studies 7. Release kinetics
  • 18. 1 8 -The microparticles drug delivery system is a physical approach to alter and improve the pharmacokinetic and pharmacodynamics properties of various types of drug molecules. -The microparticles offers a variety of opportunities such as protection and masking, better process ability, improve bioavailability, decreasing dosing frequency, improve stability, 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.
  • 19. 1 9 • As the primary and more promising fields, microparticles are utilized in composites, paints and coatings, oil and gas exploration, adhesives, cosmetics and personal grooming products, life sciences and biotechnology, medicine and medical devices. • Nevertheless, microparticles are still an area of ongoing research efforts, and outstanding work continues to be produced by researchers in this field. • One useful discovery made from the research of microspheres is a way to fight cancer on a molecular level.
  • 20. 2 0 •Pavan Kumar, B., Sarath Chandiran, I., Bhavya, B., & Sindhuri, M. (2011). Microparticulate drug delivery system: a review. Indian J Pharm Sci Res, 1(1), 19-37. • Sharma, P. (2016). Microparticles drug delivery system: a review. World J Pharm and Pharma Sci. 5(3), 543-566. •Madhav, N. S., & Kala, S. (2011). Review on microparticulate drug delivery system. Int J PharmTech Res, 3, 1242-54. •Gattani, Y. S. (2010). Floating Multiparticulate drug delivery systems: an overview. International Journal of Pharma and Bio Sciences, 1(2), 1-14. •Dubey, R. (2009). Microencapsulation technology and applications. Defence Science Journal, 59(1), 82. •James Swar Brick, James E. Boylan, Mercel dekkar. Microencapsulation technology and applications. Encyclopedia of pharmaceutical Technology,10, 1988, 245-286. •Krishna, R. S. M., Shivakumar, H. G., Gowda, D. V., & Banerjee, S. (2006). Nanoparticles-a novel colloidal drug delivery system. Indian Journal of Pharmaceutical Education and Research, 40(1), 15. •Tuncer Degim, I., & Çelebi, N. (2007). Controlled delivery of peptides and proteins. Current pharmaceutical design, 13(1), 99-117. •Alagusundaram, M., Chetty, M. S., Umashankari, K., Badarinath, A. V., Lavanya, C., & Ramkanth, S. (2009). Microspheres as a novel drug delivery system-a review. Int J Chem Tech Res, 1(3), 526-34. .
  • 21. 2 1 •Sah, H. K., Toddywala, R., & Chien, Y. W. (1995). Biodegradable microcapsules prepared by aw/o/w technique: effects of shear force to make a primary w/o emulsion on their morphology and protein release. Journal of microencapsulation, 12(1), 59-69. •Goto, S., Moriya, F., Kawata, M., & Kimura, T. (1984). Preparation and biopharmaceutical evaluation of microcapsules of amoxicillin. Journal of microencapsulation, 1(2), 137-155. •Kristl, A., Bogataj, M., Mrhar, A., & Kozjek, F. (1991). Preparation and evaluation of ethylcellulose microcapsules with bacampicillin. Drug development and industrial pharmacy, 17(8), 1109-1130. •Hoyer, H., Schlocker, W., Krum, K., & Bernkop-Schnürch, A. (2008). Preparation and evaluation of microparticles from thiolated polymers via air jet milling. European Journal of Pharmaceutics and Biopharmaceutics, 69(2), 476-485. •Lu, Z., Tsai, M., Lu, D., Wang, J., Wientjes, M. G., & Au, J. L. S. (2008). Tumor- penetrating microparticles for intraperitoneal therapy of ovarian cancer. Journal of Pharmacology and Experimental Therapeutics, 327(3), 673-682. •Naikwade, S. R., Bajaj, A. N., Gurav, P., Gatne, M. M., & Soni, P. S. (2009). Development of budesonide microparticles using spray-drying technology for pulmonary administration: design, characterization, in vitro evaluation, and in vivo efficacy study. AAPS PharmSciTech, 10(3), 993-1012. .
  • 22. 2 2 •Parida, K. R., Panda, S. K., Ravanan, P., Roy, H., Manickam, M., & Talwar, P. (2013). Microparticles based drug delivery systems: preparation and application in cancer therapeutics. Cellulose, 17, 18. •Onishi, H., & Machida, Y. (2008). In vitro and in vivo evaluation of microparticulate drug delivery systems composed of macromolecular prodrugs. Molecules, 13(9), 2136- 2155. •Sahil, K., Akanksha, M., Premjeet, S., Bilandi, A., & Kapoor, B. (2011). Microsphere: A review. Int. J. Res. Pharm. Chem, 1(4), 1184-98. •Padalkar, A. N., Shahi, S. R., & Thube, M. W. (2011). Microparticles: an approach for betterment of drug delivery system. Int J Pharm Res Dev, 1, 99-115. •Kumar, M. N. V. R. (2000). Nano and microparticles as controlled drug delivery devices. J. Pharm. Pharm. Sci, 3(2), 234-258. •http://www.omicsonline.org/open-access/microparticles-a-novel-approach-to- enhance-drug-bioavailability-jbb-10000e68.php?aid=56334#PDF. (accessed on 24/10/2016) •https://www.tri.edu.au/trans-dermal-drug-delivery-using-elongated-microparticles. (accessed on 05/11/2016) •http://www.sciencedirect.com/science/jrnlallbooks/all/open-access. (accessed on 28- 10-2016) •https://www.ncbi.nlm.nih.gov/pubmed . (accessed on 28-10-2016)
  • 23. 2 3