提高牛血清白蛋白聚乳酸聚乙醇酸微球包封率的处方筛选  

Preparation optimization about bovine serum albumin entrapment efficiency of poly lactic acid glycolic acid microspheres

作　　者：李姝瑾[1] 罗宇燕[2] 黎呐[1] 杜鹏阳[1] 张永明[2] 

机构地区：[1]中山大学药学院,广东广州510006 [2]中山大学附属第三医院,广东广州510630

出　　处：《广东药学院学报》2012年第6期588-592,共5页Academic Journal of Guangdong College of Pharmacy

基　　金：广东省重大专项科技计划项目(2011A080504003)

摘　　要：目的单因素考察蛋白药物聚乳酸聚乙醇酸(PLGA)微球包封率的不同影响因素,研究其影响机制,最后得到包封率较高的微球。方法利用海藻酸钠和CaCl2形成海藻酸钙多聚物凝胶的原理,以PLGA为药物载体,牛血清白蛋白(BSA)为模型蛋白,采用复乳化-溶剂挥发法制备微球。分别考察有机相中PLGA质量浓度、初乳匀浆时间及转速、固化时间、内水相中海藻酸钠质量浓度、外水相2体积、外水相2中CaCl2质量浓度对微球包封率的影响。结果有机相中PLGA质量浓度、初乳匀浆时间及转速、外水相2的体积、外水相2中CaCl2质量浓度对微球包封率的影响有统计学意义,而固化时间、内水相中海藻酸钠质量浓度对包封率的影响无统计学意义。选择各优选条件制备得到的微球包封率为(90.78±0.06)%。结论本研究显著提高了微球的包封率,且微球理化性质良好。Objective To study the mechanism of different influence factors on the entrapment efficiency of poly lactic acid glycolic acid（PLGA） microspheres,and optimize the preparation of microspheres with high entrapment efficiency.Methods A modified double-emulsion method was chosen,which was based on the principal that sodium alginate combined with calciumion produces ionic interaction to form a kind of sustained-release gel.Bovine serum albumin（BSA） was used as model drug,while PLGA as carrier material.PLGA concentration in organic phase,different rotational speed and time during the emulsifying process,different solidifying time,volume and calcium chlorine concentration in external water phase 2 and sodium alginate concentration in internal water phase had been studied to value the influence on the entrapment efficiency.Results It has been proved that PLGA concentration in organic phase,different rotational speed and time during the emulsifying process,volume and calcium chlorine concentration in external water phase 2 could affect the entrapment efficiency apparently.Different solidifying time and sodium alginate concentration in the internal water phase showed little difference.Entrapment efficiency of microspheres produced from modified prescribing technology was（90.78±0.06）%.Conclusion This paper optimized preparation conditions of BSA PLGA microspheres and improved the encapsulation efficiency of microspheres effectively.

关 键 词：蛋白微球 聚乳酸聚乙醇酸 海藻酸钠 包封率 

分 类 号：R944[医药卫生—药剂学]