重组人血管内皮抑制素的聚集稳定性及其PLGA缓释微球的制备与体外释放

Stability of rh-endostatin and fabrication/release test of rh-endostatin loaded PLGA microspheres

目的:制备重组人血管内皮抑制素(rh-endostatin,rh-Endo)的聚乳酸-羟基乙酸[poly(lactic-co-glycolic acid),PLGA]微球,并对微球的体外释放特性进行考察。方法:以聚乳酸-羟基乙酸为载体,采用复乳法制备重组人血管内皮抑制素聚乳酸-羟基乙酸微球,建立了高效液相色谱法测定rh-Endo含量和体外释药量。结果:微球外观圆整,平均粒径122.7μm,载药量为1.28%,包封率为38.65%,250μg/ml的rh-Endo标准溶液4℃、室温条件下放置108h后,溶液仍呈现较好的稳定性。28d的体外释放可达67.37%。结论:以可生物降解的PLGA作为载体材料,能够将rh-Endo制成缓释微球。

Objective：To prepare rh-endostatin loaded poly（lactic-co-glycolic acid）（PLGA）microspheres and to evaluate their release behavior in vitro.Methods：Rh-endostatin PLGA microspheres were prepared by W/O/W process.The content and in vitro cumulative release was determined by a HPLC method.Results：The prepared microspheres were well-shaped,with a mean diameter of 122.7 μm.The drug loading and encapsulation efficiency were 1.28% and 38.65%,respectively.The rh-Endo solution（250 μg/ml）showed good stability after placed at 4℃ and 25℃ for 108 h.The cumulative in vitro release was up to 67.37% in 28 days.Conclusion：The rh-Endo can be encapsulated in microspheres to yield sustained release using biodegradable polymers PLGA as the carrier material.