Abstract:

Aim This study was to prepare cyclosporine A (CyA) microspheres (Ms) using 75:25 poly (D, L-lactide-co-glycolide) polymer (PLGA), and to evaluate the in vitro release of the CyA microspheres. Methods CyA-Ms were prepared by an oil-in-water (o/w) emulsion solvent extraction/evaporation process and characterized for drug content, particle size, surface morphology, and differential scanning calorimeter (DSC). Accelerated in vitro release of cyclosporine A from the micropsheres was studied at various conditions, such as temperatures, surfactants, pH values and organic solvents for a short period. Results CyA-Ms were in spherical shape with average particle size of 50 μm and loading efficiency of 13.0%. The results of DSC measurements suggested that at the dry state, CyA did interact very strongly with the hydrophilic PLGA polymer. In vitro release test in various release medium showed slight increase of CyA-Ms release profiles under various conditions of temperatures, surfactants and pH values. However, dramatical increase of CyA-Ms release was seen in the medium containing 30% isopropanol. Conclusion It was demonstrated that CyA could be incorporated into polymeric Ms prepared from PLGA using a solvent evaporation technique. The release medium containing 30% isopropanol might be the ideal condition for CyA-PLGA microspheres in vitro quality control test.

Key words: Cyclosporine A CyA, Cyclosporine A CyA, Microspheres Ms, Microspheres Ms, PLGA, PLGA, In vitro release, In vitro release