3-羥基丁酸酯與3-羥基戊酸酯共聚物微粒製備與藥物制放

Abstract

Microspheres of 3-hydroxybutyrate and 3-hydroxyvalerate copolymers (PHBV) containing bovine serum albumin (BSA) were prepared using double emulsion (W1/O/W2) solvent evaporation method. Temperature of emulsification, stirring velocity, concentrations of BSA and PHBV, and species of surfactants were varied for microsphere preparation. Yields of different preparation methods, BSA incorporation efficiency, average microsphere diameter, surface morphology of microspheres and BSA delivery were investigated. BSA incorporation efficiency and average diameter of microspheres were not influenced by emulsification temperatures and stirring velocities in preparation. Higher BSA concentration used in microsphere preparation would not cause higher BSA incorporation. Higher PHBV concentration, polyvinyl alcohol(PVA) and sorbitan monooleate(Span 80) used as surfactants, applied in preparation gave higher yield and larger average diameter of microspheres. Higher concentrations of PVA and Span 80 used in formulation produced microspheres with lower BSA incorporation and average diameter. Both PVA and Span 80 used in preparation would give microspheres with much smooth surface. The use of Pluronic F-68 (PF-68) surfactant lowered BSA incorporation efficiency of microspheres. The cumulative BSA release curves for microspheres showed two stages, a burst release and a slow release. Microspheres with different formulations would cause different level of burst release in two days. Microspheres prepared with both PVA and Span 80 surfactants displayed extensive release character in 10 days, and surface porosity of microspheres was believed to be the major reason of BSA release.