超声法制备齐多夫定碳酸胆固醇酯牛血清白蛋白纳米粒  

Preparation of cholesteryl carbonate azidothymidine bovine serum albumin nanoparticles by ultrasonication technique

作　　者：石莉[1] 邓意辉[1] 董晓辉[1] 卢懿[1] 周欣羽[1] 王宁[1] 

机构地区：[1]沈阳药科大学药学院,辽宁沈阳110016

出　　处：《沈阳药科大学学报》2008年第10期759-764,共6页Journal of Shenyang Pharmaceutical University

基　　金：国家自然科学基金资助项目(30371694)

摘　　要：目的建立一种不使用交联剂制备白蛋白纳米粒的新方法。方法以牛血清白蛋白(bovineserumalbumin,BSA)为材料,以本实验室合成的齐多夫定的前药—齐多夫定碳酸胆固醇酯(cholesteryl carbonate azidothymidine,AZTC)为主药,采用超声法制备齐多夫定碳酸胆固醇酯牛血清白蛋白(AZTC-BSA)纳米粒及其冻干制剂。以粒径为考察指标确定纳米粒的最佳处方及工艺;以冻干制剂外观、水化时间及复溶后粒径为考察指标确定冻干制剂的处方及工艺。结果成功制备了AZTC-BSA纳米粒,最佳超声时间为6 min,纳米粒平均粒径为137.9 nm,zeta电位为-54.6 mV,包封率为98.6%;冻干制剂外观良好,复溶后平均粒径为148.9 nm。结论超声法制备AZTC-BSA纳米粒新颖、简单、可靠。Objective To prepare cholesteryl carbonate azidothymidine-bovine serum albumin（AZTC-BSA） nanoparticles by ultrasonication, and investigate the main factors in the process of preparing AZTC-BSA nanoparticles. Methods BSA as material, self-made AZTC which was the prodrug of AZT as the active component, AZTC-BSA nanoparticles and the freeze-dried formulations were successfully prepared by ultrasonication. The optimum formulation was selected through the mean particle size of AZTC-BSA nanopartilces. The appearance, rehydration time and particle size were also investigated to optimize the formulation of nanoparticles freeze-dried. Results The mean diameter of AZTC-BSA nanopartilces was 137.9 nm, the zeta potential was - 54.6 mV, and the encapsulation efficiency was 98.6 %. The mean diameter of nanopartilces freeze-dried with good appearance was 148.9 nm. Conclusions The technique of preparing AZTC-BSA nanoparticles with ultrasonication is simple, reliable and novel.

关 键 词：齐多夫定碳酸胆固醇酯 牛血清白蛋白 纳米粒 超声法 冻干保护剂 粒径分布 

分 类 号：R94[医药卫生—药剂学]