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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
王明娟1,张翮1,鲁莹1,邹豪1,张锋2,陈华江2,王江峰1,钟延强1*
0
(1.第二军医大学药学院药剂学教研室,上海 200433*2.第二军医大学长征医院骨科,上海 200003)
摘要:
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122.7 μm,载药量为1.28%,包封率为38.65%,250 μg/ml的rh-Endo标准溶液4℃、室温条件下放置108 h后,溶液仍呈现较好的稳定性。28 d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。
关键词:  重组人血管内皮抑制素  稳定性  聚乳酸-羟基乙酸  微球
DOI:10.3724/SP.J.1008.2009.00028
投稿时间:2008-07-10修订日期:2008-11-25
基金项目:
Stability of rh-endostatin and fabrication/release test of rh-endostatin loaded PLGA microspheres
WANG Ming-juan1, ZHANG He1, LU Ying1, ZOU Hao1, ZHANG Feng2, CHEN Hua-jiang2, WANG Jiang-feng1, ZHONG Yan-qiang1*
(1.Department of Pharmaceutics, School of Pharmacy, Second Military Medical University, Shanghai 200433, China*2.Department of Orthopaedics, Changzheng Hospital, Second Military Medical University, Shanghai 200003)
Abstract:
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.
Key words:  rh-endostatin  stability  poly(lactic-co-glycolic acid)  microspheres