【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。更多还原

【Abstract】 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.更多还原