脂质体辅料磷脂酰甘油类分子的合成研究进展  

Research progress in synthesis of liposome excipients phosphatidylglycerol molecules

作　　者：董玉洁 刘耀文 陈舒旸 DONG Yu-jie;LIU Yao-wen;CHEN Shu-yang(China State Institude of Pharmaceutical Industry,Shanghai 201203,China)

机构地区：[1]中国医药工业研究总院,上海201203

出　　处：《中国药物化学杂志》2023年第5期380-385,共6页Chinese Journal of Medicinal Chemistry

摘　　要：磷脂酰甘油类分子是甘油酯类衍生物,广泛应用于脂质体药物、脂质纳米颗粒(LNP)药物递送系统、小干扰核糖核酸(siRNA)药物等。本文作者基于对文献的总结以及对磷脂的结构分析,综述了磷脂酰甘油类分子的两种合成途径,即生物方法和化学方法。其中生物方法以磷脂酶D催化反应为主,化学方法主要包括两个片段的构建:由甘油衍生物合成二酰甘油酯,以及磷脂头部基团的构建。随着新型制剂的发展,磷脂酰甘油类分子作为核心辅料具有广阔的市场应用前景。Phosphatidylglycerol molecules have been widely used in liposome drugs,LNP drug delivery systems,siRNA drugs,etc.as core excipients.Based on the summary of literatures and the structural analysis of phospholipids,two synthetic approaches of phosphatidylglycerol molecules,biological and chemical methods,were reviewed in detail.Among them,the biological method is mainly enzyme catalyzed reaction,and the chemical method divides the molecular structure into two parts.Phosphatidylglycerols molecules as high-end pharmaceutical excipients have a good market prospect.

关 键 词：磷脂酰甘油 生物合成 化学合成 脂质体辅料 

分 类 号：R914[医药卫生—药物化学]