Preparation, characterization and in vitro release study of BSA-loaded double-walled glucose-poly(lactide-co-glycolide) microspheres

Arch Pharm Res. 2016 Sep;39(9):1242-56. doi: 10.1007/s12272-016-0710-3. Epub 2016 Jan 27.

Abstract

The aim of this study was to prepare a model protein, bovine serum albumin (BSA) loaded double-walled microspheres using a fast degrading glucose core, hydroxyl-terminated poly(lactide-co-glycolide) (Glu-PLGA) and a moderate-degrading carboxyl-terminated PLGA polymers to reduce the initial burst release and to eliminate the lag phase from the release profile of PLGA microspheres. The double-walled microspheres were prepared using a modified water-in-oil-in-oil-in-water (w/o/o/w) method and single-polymer microspheres were prepared using a conventional water-in-oil-in-water (w/o/w) emulsion solvent evaporation method. The particle size, morphology, encapsulation efficiency, thermal properties, in vitro drug release and structural integrity of BSA were evaluated in this study. Double-walled microspheres prepared with Glu-PLGA and PLGA polymers with a mass ratio of 1:1 were non-porous, smooth-surfaced, and spherical in shape. A significant reduction of initial burst release was achieved for the double-walled microspheres compared to single-polymer microspheres. In addition, microspheres prepared using Glu-PLGA and PLGA polymers in a mass ratio of 1:1 exhibited continuous BSA release after the small initial burst without any lag phase. It can be concluded that the double-walled microspheres made of Glu-PLGA and PLGA polymers in a mass ratio of 1:1 can be a potential delivery system for pharmaceutical proteins.

Keywords: Controlled release; Drug delivery; Encapsulation efficiency; Microspheres; Poly(lactide-co-glycolide); Therapeutic proteins.

MeSH terms

  • Animals
  • Cattle
  • Drug Liberation*
  • Glucose / chemical synthesis*
  • Glucose / metabolism
  • Lactic Acid / chemical synthesis*
  • Lactic Acid / metabolism
  • Microspheres*
  • Particle Size
  • Polyglycolic Acid / chemical synthesis*
  • Polyglycolic Acid / metabolism
  • Polylactic Acid-Polyglycolic Acid Copolymer
  • Serum Albumin, Bovine / chemical synthesis*
  • Serum Albumin, Bovine / metabolism

Substances

  • Polylactic Acid-Polyglycolic Acid Copolymer
  • Polyglycolic Acid
  • Serum Albumin, Bovine
  • Lactic Acid
  • Glucose