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The Effect of Formulation Variables on the Characteristics of Insulin-Loaded Poly(Lactic-Co-Glycolic Acid) Microspheres Prepared by a Single Phase Oil in Oil Solvent Evaporation Method Publisher Pubmed



Hamishehkar H1 ; Emami J2 ; Najafabadi AR3 ; Gilani K3 ; Minaiyan M2 ; Mahdavi H4 ; Nokhodchi A5
Authors
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Authors Affiliations
  1. 1. Pharmaceutical Technology Laboratory, Drug Applied Research Center, Tabriz University (Medical Sciences), Tabriz, Iran
  2. 2. School of Pharmacy and Pharmaceutical Sciences, Isfahan Pharmaceutical Research Center, Isfahan University of Medical Sciences, Isfahan, Iran
  3. 3. Aerosol Research Laboratory, School of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran
  4. 4. Department of Novel Drug Delivery Systems, Iran Polymer and Petrochemical Institute, Tehran, Iran
  5. 5. Medway School of Pharmacy, The Universities of Kent and Greenwich, Chatham Maritime ME4 4TB, Kent, Central Ave, United Kingdom

Source: Colloids and Surfaces B: Biointerfaces Published:2009


Abstract

Biodegradable polymeric microspheres are ideal vehicles for controlled delivery applications of drugs, peptides and proteins. Amongst them, poly(lactic-co-glycolic acid) (PLGA) has generated enormous interest due to their favorable properties and also has been approved by FDA for drug delivery. Insulin-loaded PLGA microparticles were prepared by our developed single phase oil in oil (o/o) emulsion solvent evaporation technique. Insulin, a model protein, was successfully loaded into microparticles by changing experimental variables such as polymer molecular weight, polymer concentration, surfactant concentration and stirring speed in order to optimize process variables on drug encapsulation efficiency, release rates, size and size distribution. A 24 full factorial design was employed to evaluate systematically the combined effect of variables on responses. Scanning electron microscope (SEM) confirmed spherical shapes, smooth surface morphology and microsphere structure without aggregation. FTIR and DSC results showed drug-polymer interaction. The encapsulation efficiency of insulin was mainly influenced by surfactant concentration. Moreover, polymer concentration and polymer molecular weight affected burst release of drug and size characteristics of microspheres, respectively. It was concluded that using PLGA with higher molecular weight, high surfactant and polymer concentrations led to a more appropriate encapsulation efficiency of insulin with low burst effect and desirable release pattern. © 2009 Elsevier B.V. All rights reserved.
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