聚乳酸乙醇酸的生物降解和安全性研究进展.pdfVIP

• 422 • 现代药物与临床 Drugs Clinic 第 27 卷 第 4 期 2012 年 7 月 聚乳酸乙醇酸的生物降解和安全性研究进展 韦宝伟，刘布鸣* 广西中医药研究院 广西中药质量标准研究重点实验室，广西 南宁 530022 摘 要：聚乳酸乙醇酸（PLGA ）的降解主要是通过酯键水解，自催化作用和巨噬细胞吞噬；水解产物为乳酸和乙醇酸，均 可代谢分解生成二氧化碳和水，分别通过肺和肾排出体外，仅有微量的原型聚合物经尿液排出，体内没有蓄积现象。PLGA 具有良好的生物相容性和可生物降解性，作为组织工程支架和药物控释系统材料是安全的。美国食品药品管理局（FDA ）已 经批准将 PLGA 作为组织工程细胞支架和药物载体，在美国、日本市场应用多年，未见严重的不良反应报道。目前国产PLGA 的质量和控释微球药品的开发研究仍需要提高，尤其是制剂的载药量、控释技术以及稳定性技术。介绍 PLGA 的生物降解 与安全性研究进展，为开发 PLGA 控释系统提供参考。 关键词：聚乳酸乙醇酸；体内代谢；生物降解；安全性 中图分类号：R943 文献标志码：A 文章编号：1674 - 5515(2012)04 - 0422 - 07 Advances in studies on biodegradation and safety of poly lactic-co-glycolic acid WEI Bao-wei, LIU Bu-ming Guangxi Key Laboratory of Traditional Chinese Medicine Quality Standards, Guangxi Institute of Chinese Medicine Pharmaceutical Science, Nanning 530022, China Abstract: Poly lactic-co-glycolic acid (PLGA) is biodegraded mainly through hydrolysis of its ester linkages, self-catalysis, or phagocytosis by macrophage. Lactic acid and glycolic acid, the products of hydrolysis process, are then eventually catabolized into carbon dioxide and water which are eliminated via lungs and kidneys, respectively. Only trace PLGA is excreted in urine. No accumulation of PLGA is found in the body. PLGA showed excellent biocompatibility and biodegradability, so it is safe for using as materials for scaffolds of tissue engineering and drug controlled release system, and the US Food and Drug Administration (FDA) has approved its use for preparation of scaffolds for tissue engineering and carrier of drug. It has been used in the market in United States and Japan for many years, and no serious side effects have been reported. At present, the quality of domestic PLGA and the development of drug controlled release system with