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PLGA微粒中蛋白稳定性和完全释放的研究进展
张敏1,高静2,张玮3,高申1*
0
(1. 第二军医大学长海医院药学部,上海 200433
2. 第二军医大学药学院药剂学教研室,上海 200433
3. 解放军第522医院药械科,洛阳 471000
*通信作者)
摘要:
以PLGA为载体的蛋白药物微粒给药系统存在的最大的问题是蛋白稳定性和蛋白的完全释放。本文总结了增强蛋白药物稳定性和在体外释放期间促使蛋白完全释放的方法 。蛋白药物完全释放的前提是保持蛋白稳定性。保持蛋白稳定性的方法 之一是通过加入添加剂、对蛋白药物和聚合物进行修饰等避免蛋白在不利释放环境中聚集变性;另一个方法 是避免不稳定环境的形成。
关键词:  蛋白  PLGA微粒  稳定性  药物释放系统
DOI:10.3724/SP.J.1008.2012.00328
基金项目:
Stability and complete release of protein from PLGA-based microparticles: an update
ZHANG Min1,GAO Jing2,ZHANG Wei3,GAO Shen1*
(1. Department of Pharmaceutics, Changhai Hospital, Second Military Medical University, Shanghai 200433, China
2. Department of Pharmaceutics, School of Pharmacy, Second Military Medical University, Shanghai 200433, China
3. Department of Pharmaceutics, No. 522 Hospital of PLA, Luoyang 471000, Henan, China
*Corresponding author.)
Abstract:
One of the most challenging issues in the delivery of therapeutic proteins from PLGA-based microparticles is the stability and complete release of the protein in its native form. This review summarizes the methods to promote the stability and in vitro release of protein from PLGA-based microparticles. Protein stability is the precondition of complete release. One way to keep protein stability is to use stabilizer or modify protein to avoid denaturation and aggregation; another way is to avoid the pro-instability environment.
Key words:  protein  PLGA microspheres  stability  drug delivery systems