胰高血糖素样肽-1缓释微球技术进展  

Advances in the preparation technology of sustained-release microspheres of glucagon-like peptide-1(GLP-1)

作　　者：刘波 阮思达 蔡挺 LIU Bo;RUAN Si-da;CAI Ting(Department of Pharmaceutics,China Pharmaceutical University,Nanjing 210009,China;State Key Laboratory of Natural Medicines,China Pharmaceutical University,Nanjing 210009,China)

机构地区：[1]中国药科大学药学院药剂系,南京210009 [2]中国药科大学天然药物活性组分与药效国家重点实验室,南京210009

出　　处：《中国新药杂志》2021年第13期1184-1191,共8页Chinese Journal of New Drugs

基　　金：国家“重大新药创制”科技重大专项资助项目(2017XZ09301075);国家自然科学基金资助项目(81872813);中国药科大学“双一流”建设项目(CPU2018GY13)。

摘　　要：胰高血糖素样肽-1(GLP-1)是一种新型的具有血糖响应性质的降糖多肽,也为2型糖尿病的治疗提供了新的药物选择。然而GLP-1多肽的半衰期较短(约1~2 min),因此也限制了该多肽作为药物的应用。通过微球技术实现GLP-1的缓释治疗近年来受到了广泛关注。本文介绍了聚乳酸-聚羟基乙酸(PLGA)缓释微球用于包载GLP-1的制备方法,并且针对传统PLGA微球载药时面临的突释较大以及药物降解等问题,对新型的缓释微球技术(双层微球、自愈合多孔微球以及其他新型微球制剂)进行总结。这些新型微球技术能够有效提高蛋白药物的稳定性并能够得到长效的治疗效果,为蛋白类药物缓释微球的开发提供了新策略。Glucagon-like peptide-1(GLP-1),considered as an effective peptide for the treatment of diabetes,can stimulate insulin secretion in response to rising glucose.Moreover,the novel peptide is becoming a new choice to treat type II diabetes.Nevertheless,the half-life of GLP-1(approximately 1~2 min)is short,limiting its clinical application in diabetes.GLP-1-loaded PLGA microspheres have drawn more attentions in recent years.In this article,we introduces the preparation methods for encapsulation of GLP-1 in preparing PLGA microspheres.In order to solve the shortcomings of large burst release and drug degradation of traditional microspheres,some novel microsphere formulations(double-wall microspheres,self-healing microspheres and other new formulations of microspheres)are summarized.The new formulations effectively enhance protein stability and long-acting efficiency is achieved,providing new strategies for developing protein-loaded microspheres.

关 键 词：胰高血糖素样肽-1 聚乳酸-聚羟基乙酸 微球 缓释 

分 类 号：R944.9[医药卫生—药剂学]