脂质体主动载药技术研究进展  

A review on progress involving remote loading for liposomes preparation

作　　者：顾华芳 徐歌 朱柯武 沈润溥[1] 席眉扬 周艳艳 骆翔 GU Huafang;XU Ge;ZHU Kewu;SHEN Runpu;XI Meiyang;ZHOU Yanyan;LUO Xiang(Shaoxing University,Shaoxing 312000,China;Novus Pharmaceuticals Co.,Ltd.,Shaoxing 312500,China)

机构地区：[1]绍兴文理学院,浙江绍兴312000 [2]浙江创新生物有限公司,浙江绍兴312000

出　　处：《中国药剂学杂志》2021年第6期173-185,共13页Chinese Journal of Pharmaceutics

基　　金：浙江省博士后科研择优资助项目(ZJ2021024);2020绍兴文理学院校级科研项目(2020LG1002);2019年浙江省大学生科技创新活动计划暨新苗人才计划(2019R432014)。

摘　　要：目的为了提高脂质体药物递送系统中药物的包封率和稳定性,脂质体主动载药技术被成功开发并应用于脂质体产品,本文对脂质体主动载药技术的发展历史及最新进展进行综述。方法通过对近年来报道的近百篇脂质体主动载药技术相关文献整理,着重对影响主动载药的几个共性关键条件进行了分析和讨论。结果本文主要综述了跨膜梯度、载药温度和时间、药脂比、外水相pH调节剂、内水相缓冲能力、药物Log P值和pKa值等主动载药共性关键条件对脂质体药物递送系统中药物的包封率和稳定性的影响。结论主动载药技术作为一种制备脂质体药物递送系统最重要的方法,通过不断深入研究其技术规律,阐明其共性关键条件,必将推动脂质体药物递送系统的产业化进程。Purpose In order to improve the encapsulation efficiency and stability of liposomal drug delivery systems,the remote loading technique has been successfully developed and applied to liposomes preparation.The paper presents a review on the history and progress o f remote loading technique being used for the preparation of liposomes.Method A total of 101 publications of the remote loading technique were examined.Several key general characteristics of the remote loading technique were analyzed and discussed,which will have important effect on the encapsulation efficiency and stability of liposomes,such as transmembrane gradient,drug-loading temperature and time,drug-lipid ratio,pH adjuster,buffering capacity in internal water phase,Log P value and pKa value of drug,and so on.Results As a most important method for liposome preparation,the remote loading technique will promote the industrialization process of liposome by continuously investigating and clarifying its technical rules and key general characteri stics.

关 键 词：脂质体 主动载药 包封率 稳定性 跨膜离子梯度 

分 类 号：R94[医药卫生—药剂学]