乳酸-羟基乙酸共聚物缓释微球的制备工艺与生物学性能

Preparation technique and biological performance of poly(lactic-co-glycolic acid) sustained-release microspheres

微球(microspheres)是一种生物物理靶向载药制剂,粒径为1～300μm。微球的载体材料按其来源可分为天然高分子材料、半合成高分子材料及合成高分子材料。在合成高分子材料中,通过采用合适的制备工艺和处方,制得的载药微球可在几周或几个月时间内以一定速率释放药物,减少给药次数,增加患者顺应性。对蛋白和多肽类药物,微球是相当理想的载药系统。微球制剂是近年来缓释剂型的研究热点,根据临床需要很多药物正被研究成微球制剂。乳酸-羟基乙酸共聚物[poly(lactic-co-glycolic acid),PLGA]有着优良的安全性、生物相容性和可变的生物降解性,是制备微球的常用基本材料。PLGA缓释微球制剂的制备方法基本上可分为3种:溶剂挥发法、喷雾干燥法、相分离法。溶剂挥发法是常用的制备方法之一,目前PLGA微球作为多肽、蛋白类药物的载体已广泛应用于免疫学、基因治疗、肿瘤治疗、骨缺损修复、眼科等众多医学领域中。

Microsphere of diameter 1 300μm is a biophysical target drug-loading reagent. Loading material of microspheres is classified into natural polymer, semisynthetic macromolecule, and synthetic macromolecule. Based on proper preparation technique and prescription, drug-loading microspheres made by synthetic macromolecule can release drug to a certain velocity during several weeks or months, reduce administration times, and enhance complaisance. Moreover, microspheres are ideal drug-loading system for protein and polypeptide drug. Research of microspheres is e hot topic at recent, thus more and more drugs are developed into microspheres. Poly0actic-co-glyc, olic acid） （PLGA） characterizing by great security, good biocompatibility, and alterable biodegradation is a common material to make microspheres. There are three ways to establish PLGA sustained-release microspheres, including solvent evaporation method, spray drying method, and phase separation method. In particular, solvent evaporation method is frequently used to make PLGA microspheres loading polypeptide and protein in various medical fields of immunology, gene therapy, tumor therapy, bone defect repairing, and ophthalmology.