摘要
目的以紫杉醇为难溶性药物模型,制备自组装紫杉醇白蛋白纳米粒。方法谷胱甘肽作为还原剂,经细胞超声制备白蛋白纳米粒,通过正交试验筛选出最优处方。结果结果表明BSA浓度为1.5 g·L-1,谷胱甘肽用量为90 mg,紫杉醇/白蛋白质量比为1:20时,可以制备出表面圆整,粒径为91.19 nm,zeta电位-12.8 mv,包封率为90.8%,载药量为4.5%的紫杉醇白蛋白纳米粒,体外药物释放符合peppas模型,n=0.29,主要以扩散释药为主。结论自组装法制备出的白蛋白纳米粒粒径均一可控,并可显著提高白蛋白对难溶性药物的包封率。
Objective To fabricate albumin nanoparticles through self-assembly of BSA, using paclitaxel as a model drug. Methods Glutathione was applied as reducing agent to prepare albumin nanoparticles through ultrasonic cell disrupting, and orthogonal design was used to optimize the formulation. Results Spherical paclitaxel albumin nanoparticles were made with mean particle size 91.19 nm, Zeta potential-12.8 mv, drug entrapment efficiency 90.8% and drug loading 4.5%.The mechanism of release was drug diffusion from matrix by fitting drug release data with Peppas model. Conclusion Albumin-bound hydrophobic drug nanoparticles with controlled particle size and high encapsulation efficiency were obtained through self-assembly method.
出处
《中国药剂学杂志（网络版）》
2014年第4期17-24,共8页
Chinese Journal of Pharmaceutics：Online Edition
关键词
药剂学
白蛋白纳米粒
自组装
紫杉醇
粒径
pharmaceutics
albumin nanoparticles
self-assembly method
paclitaxel
particle diameter
