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缓释微粒给药系统是蛋白质/多肽药物传输系统的一个重要研究方向,聚乳酸和乳酸-羟基乙酸共聚物是制备缓释微球最常用的载体材料。蛋白质/多肽药物聚乳酸/乳酸-羟基乙酸共聚物微球常用的制备方法包括溶剂萃取/挥发法(复乳法)、相分离法和喷雾干燥法。本文总结了微球制备中面临的难点如蛋白质/多肽药物稳定性、包封率、药物突释和药物吸附等问题,并综述了保持药物结构稳定性和生物活性、提高包封率、改善药物释放曲线等微球制备方法和进展。
Sustained-release microparticle drug delivery system is an important research direction of protein / peptide drug delivery system. Polylactic acid and lactic acid-glycolic acid copolymer are the most commonly used carrier materials for preparing sustained-release microspheres. Commonly used preparation methods of protein / polypeptide drugs polylactic acid / lactic acid-glycolic acid copolymer microspheres include solvent extraction / volatilization (double emulsion method), phase separation and spray drying. This article summarizes the difficulties encountered in the preparation of microspheres such as protein / peptide drug stability, entrapment efficiency, drug burst release and drug adsorption issues, and reviews the structural stability and biological activity of drugs to improve, improve the entrapment efficiency and improve the drug Release curve and other preparation methods and progress of microspheres.