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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。
Aim To establish a new method of preparing albumin nanoparticles without using cross-linking agent. Methods Bovine serum albumin (BSA) was used as material to synthesize zidovudine (AZTC), a zidovudine prodrug synthesized in our laboratory. Zidovudine Cholesteryl Carbonate Bovine Serum Albumin (AZTC-BSA) Nanoparticles and their Freeze-dried Formulations. The optimum prescription and technology of nanoparticles were determined by particle size. The appearance and the hydration time of the lyophilized preparation and the particle size after reconstitution were determined to determine the prescription and technology of the lyophilized preparation. Results AZTC-BSA nanoparticles were successfully prepared. The optimal ultrasonic time was 6 min, the average particle size was 137.9 nm, the zeta potential was-54.6 mV and the entrapment efficiency was 98.6%. The appearance of the lyophilized preparation was good. After reconstitution The average particle size is 148.9 nm. Conclusion Ultrasound preparation of AZTC-BSA nanoparticles is novel, simple and reliable.