Xu Feng-Hua, Zhang Qiang
Division of Pharmacology and Pharmaceutics, General Hospital of PLA, Beijing 100853, China.
Yao Xue Xue Bao. 2007 Jan;42(1):1-7.
Sustained release drug delivery from microparticles is an excellent alternative for daily protein/peptide drug administration protocol. Poly(lactic acid) (PLA) and poly(lactic-co-glycolic acid) (PLGA) are the most commonly used polymer carriers in the development of protein/peptide microspheres. Basically there are three preparation methods for PLA/PLGA microspheres: the solvent extraction/evaporation based multiple emulsion (W/O/W emulsion) method, the phase separation method and the spray drying method. The stability of the protein/pipetide loaded, encapsulation efficiency, and the burst effect of the microspheres are key problems usually met in the preparation of microspheres. In this review the preparation techniques and progress in the development of protein/pipetide microspheres which aimed to stabilize protein/peptide structural integrity, keep the bioactivity of drugs, increase the encapsulation efficiency and improve the release profile were summarized and evaluated.
从微粒进行缓释药物递送是日常蛋白质/肽类药物给药方案的一种极佳选择。聚乳酸（PLA）和聚乳酸-乙醇酸共聚物（PLGA）是蛋白质/肽微球研发中最常用的聚合物载体。基本上，PLA/PLGA微球有三种制备方法：基于溶剂萃取/蒸发的复乳（W/O/W乳液）法、相分离法和喷雾干燥法。载有蛋白质/肽的微球的稳定性、包封效率以及微球的突释效应是微球制备过程中通常会遇到的关键问题。在本综述中，总结并评估了旨在稳定蛋白质/肽结构完整性、保持药物生物活性、提高包封效率并改善释放曲线的蛋白质/肽微球的制备技术及进展。
