紫杉醇白蛋白片段纳米粒的制备

Preparation of Paclitaxel-loaded nanoparticles by albumin fragments

摘要:

目的：利用蛋白酶解和纳米粒技术在白蛋白片段的基础上筛选制备紫杉醇纳米粒的新型载体，并考察相关理化指标。方法：利用牛血白蛋白（Bovine serum albumin，BSA）酶解片段作为载体，分散乳化-旋蒸去溶剂法制备紫杉醇-BSA酶解片段-纳米粒，在外观、粒径分布、收率、包封率、载药量及体外释药性方面对样品进行考察。结果：BSA酶解后经粗分离得到4个片段组，选择第4组为候选载体，得到的纳米粒外观形态圆整、均匀，初制备纳米粒混悬剂平均粒径为150.2 nm，平均收率为（45.132±0.903）%，平均包封率为（50.246±0.712）%，平均载药量为（4.804±0.101）%，48 h累计释药82.4%。结论：利用白蛋白酶解片段制备紫杉醇纳米粒是可行的，为扩大紫杉醇纳米粒的载体来源、降低制备成本提供了可能。

Abstract:

Objective：To screen and prepare the new carrier for Paclitaxel-loaded nanoparticles from bovine serum albumin by prote－olysis and nanoparticle technology and to study the physical and chemical indicators. Methods：Bovine serum albumin（BSA） which was degraded to fragments by pepsin was used as a carrier，the Paclitaxel-BSA fragments-nanoparticles were prepared by homoge－nized-spin steam. The appearance，size distribution，yield，encapsulation efficiency，drug loading and release in vitro of the sample were assessed. Results：Four clip groups were got through column chromatography after BSA enzymolysis. The fourth group was cho－sen as the candidate carrier. The nanoparticles got were round and uniform in shape with an average diameter of 150.2 nm. The aver－age yield of nanoparticles was（45.132±0.903）%，average encapsulation efficiency was （50.246±0.712）%，average drug-loading rate was （4.804±0.101）% and the 48 h accumulative release percentage was 82.4%. Conclusions：The preparation of Paclitaxel-loaded nanoparticles through BSA enzymolysis is feasible. Therefore，there is possibility to increase the sources of carriers for Pacli－taxel-loaded nanoparticles and to reduce the cost of prepara－tion.