棉酚白蛋白纳米粒的制备及其体外释放  

Preparation of gossypol loaded BSA nanoparticles and its in vitro releasing properties

作　　者：杨四涛[1] 唐辉[1] 吴旭东[1] 陈欢[1] 刘艳芳[1] 

机构地区：[1]新疆特种植物药资源教育部重点实验室,石河子大学药学院,新疆石河子832002

出　　处：《中国医院药学杂志》2011年第18期1528-1532,共5页Chinese Journal of Hospital Pharmacy

基　　金：兵团博士基金项目(编号:2009JC14);国家教育部重点课题(编号:205815);石河子大学高层次人才科研启动资金专项(编号:RC-ZX200762)

摘　　要：目的:优化超声-溶剂沉淀法制备棉酚白蛋白纳米粒的工艺。方法:采用正交设计,以白蛋白浓度、有机相与水相比、乳化分散时间为考察因素,根据L9(34)正交设计原理安排实验,对包封率、载药量、平均粒径进行归一化处理后,再以总体的归一值为综合评价指标,优化出处方。对优化出的制剂采用透射电镜进行观察,并且进行体外释放研究拟合药物释放曲线。结果:优化的最佳条件为白蛋白浓度1%,有机相与水相比2∶25,高剪切乳化时间60 s,在此条件下制备的棉酚白蛋白纳米粒载药量为15.34%,包封率为91.21%,粒径为435 nm。结论:制备的白蛋白纳米粒体外有缓释能力,拟合方程符合Higuchi方程。OBJECTIVE TO prepare the gossypol loaded BSA nanoparticles and optimize the best condition. METHODS The method of ultrasonic-solvent disposition was used.The orthogonal experiment design method,the concentration of BSA,the volume ratio of the aqueous phase to oil and the emulsifying time was considered as factors.L9（34）experiment was arranged.Drug loading,encapsulation efficiency and mean diameter were studied and normalized as the value of 0 to 1.The optimized nanoparticles were observed under TEM and evaluated the release in vitro. RESULTS The optimal conditions were 1% albumin concentration,2∶25 the volume ratio of the aqueous phase to oil,60 s emulsifying time,under these conditions,the BSA nanoparticles could be prepared at high encapsulation efficiency with uniform particle size.In vitro release showed that GA-BSA-NP exhibited sustained release after an initial burst release. CONCLUSION The drug release from nanoparticles in vitro fitted the Higuchi equation well and had a property of sustained release.

关 键 词：棉酚白蛋白纳米粒 包封率 载药量 工艺优化 体外释药 

分 类 号：R943[医药卫生—药剂学]