艾塞那肽缓释微球的制备工艺及其体外释放特性的研究

摘要

Objective To prepare biodegradable[poly lactic-co-glycolic acid(PLGA )] microspheres containing exendin-4 and to study the drug release characteristics .Methods Exendin-4 loaded microspheres were prepared with(poly lactic-co-glycolic acid ,PLGA) as carrier materials by a double emulsion (W/O/W) method .Physical and chemical characteristics of microspheres ,such as mean diameter ,morphology and drug loading were evaluated .The release behavior in vitro was evaluated .Results Microspheres with good shape and dispersive quality were prepared .The drug entrapment efficiency was about 60% .The accumulated release in one week is up to 80% .Conclusion The optimized technology presents good stability and obvious effect of sustained drug release .%目的：制备含艾塞那肽（exendin-4）的聚乳酸-羟基乙酸共聚物（poly lactic-co-glycolic acid ，PLGA ）微球，并对制备工艺及其体外释药特性进行研究。方法采用复乳法（W／O／W ）制备ex endin-4缓释注射微球；通过考察微球粒径大小、分布、外观、载药量和包封率等理化性质，对微球的制备工艺进行了研究；并对其体外释放特性进行了考察。结果微球形态圆整、分散性好，粒径分布均一，微球的包封率在60％左右，1周累积释药可达80％以上。结论该法制备微球工艺稳定，所得微球具有显著的体外缓释效果。