Preparation and in Vitro Release Behavior of Paclitaxel Microsphere / 中国药房

ABSTRACT

OBJECTIVE:To optimize the formulation parameters of poly1,3-bis(p-carboxyphenoxy) propane-sebacic acid (P(CPP∶SA)) microsphere and evaluate its drug release performance in vitro. METHODS: The paclitaxel microspheres were prepared by single emulsion method,and the effects of the factors such as the stirring speed (A),P(CPP∶SA) concentration (B),emulsifier polyvinyl alcohol (PVA) concentration (C) on encapsulation efficiency were evaluated by orthogonal test. The surface morphology of the prepared microsphere was observed and its drug release performance in vitro was evaluated. RESULTS: The optimal formulation of the microsphere obtained was as follows A was 4 000 r?min-1,B was 80 mg?mL-1 and C was 1%,respectively. The morphology of microspheres was round and intact. The encapsulation efficiency of paclitaxel was up to above 90%. The sustained release duration was 30 days with an accumulative release rate of over 80%. CONCLUSION: Paclitaxel microspheres prepared by optimal formula display a high encapsulation efficiency and satisfactory sustained-release pattern.