Development and Characterization of Polymeric Microspheres for Controlled Release Protein Loaded Drug Delivery System

The aim of the present work was to investigate the preparation of microspheres as potential drug carriers for proteins, intended for controlled release formulation. The hydrophilic bovine serum albumin was chosen as a model protein to be encapsulated within poly(D,L-lactide-co-glycolide) (50:50) microspheres using a w/o/w double emulsion solvent evaporation method. Different parameters influencing the particle size, entrapment efficiency and in vitro release profiles were investigated. The microspheres prepared with different molecular weight and hydrophilicity of poly(D,L-lactide-co-glycolide) polymers were non porous, smooth surfaced and spherical in structure under scanning electron microscope with a mean particle size ranging from 3.98 to 8.74 μm. The protein loading efficiency varied from 40 to 71% of the theoretical amount incorporated. The in vitro release profile of bovine serum albumin from microspheres presented two phases, initial burst release phase due to the protein adsorbed on the microsphere surface, followed by slower and continuous release phase corresponding to the protein entrapped in polymer matrix. The release rate was fairly constant after an initial burst release. Consequently, these microspheres can be proposed as new controlled release protein delivery system.

[1]  H. Okada,et al.  Biodegradable microspheres in drug delivery. , 1995, Critical reviews in therapeutic drug carrier systems.

[2]  R. Bodmeier,et al.  Solvent selection in the preparation of poly(dl-lactide) microspheres prepared by the solvent evaporation method , 1988 .

[3]  M. Alonso,et al.  Protein encapsulation and release from poly(lactide-co-glycolide) microspheres: effect of the protein and polymer properties and of the co-encapsulation of surfactants. , 1998, European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V.

[4]  J. Rigelsford Handbook of Pharmaceutical Controlled release Technology , 2002 .

[5]  A. Coombes,et al.  Protein-loaded poly(dl-lactide-co-glycolide) microparticles for oral administration: formulation, structural and release characteristics , 1997 .

[6]  P. Deluca,et al.  Polymer and microsphere blending to alter the release of a peptide from PLGA microspheres. , 2000, European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V.

[7]  R. Narain,et al.  Protein encapsulation and release from degradable sugar based hydrogels , 2009 .

[8]  J. Resau,et al.  Characterization and morphological analysis of protein-loaded poly(lactide-co-glycolide) microparticles prepared by water-in-oil-in-water emulsion technique , 1994 .

[9]  O'donnell,et al.  Preparation of microspheres by the solvent evaporation technique. , 1997, Advanced drug delivery reviews.

[10]  Jagdish Singh,et al.  Effect of additives on the release of a model protein from PLGA microspheres , 2001, AAPS PharmSciTech.

[11]  U. Banakar,et al.  Implantable Drug Delivery , 1994, Journal of biomaterials applications.

[12]  J. Pedraz,et al.  Stability of BSA encapsulated into PLGA microspheres using PAGE and capillary electrophoresis , 1998 .

[13]  L. M. Sanders Drug delivery systems and routes of administration of peptide and protein drugs , 1990, European Journal of Drug Metabolism and Pharmacokinetics.

[14]  V. Sinha,et al.  Biodegradable microspheres for protein delivery. , 2003, Journal of controlled release : official journal of the Controlled Release Society.

[15]  Yi Yan Yang,et al.  Morphology, drug distribution, and in vitro release profiles of biodegradable polymeric microspheres containing protein fabricated by double-emulsion solvent extraction/evaporation method. , 2001, Biomaterials.

[16]  María J. Alonso,et al.  Development and characterization of protein-loaded poly(lactide-co-glycolide) nanospheres , 1997 .

[17]  D. Wise Microsphere Preparation by Solvent Evaporation Method , 2000 .