脂质液晶纳米分散体在缓控释药物递送系统中的研究进展  

Research Advances of Lipid Liquid Crystalline Nano-dispersions in Sustained-and Controlled-release Drug Delivery Systems

作　　者：曾馨 刘洁[1] 杨亚妮[1] 何军[1] ZENG Xin;LIU Jie;YANG Yani;HE Jun(National Pharmaceutical Engineering Research Center, China State Institute of Pharmaceutical Industry, Shanghai 201203)

机构地区：[1]中国医药工业研究总院药物制剂国家工程研究中心,上海201203

出　　处：《中国医药工业杂志》2018年第5期547-556,共10页Chinese Journal of Pharmaceuticals

基　　金：2015年上海市人才发展资金(201576)

摘　　要：两亲性脂质在特定条件下可以自组装形成不同结构的反脂质液晶相,将其分散在过量水中可得到各种结构的脂质液晶纳米分散体,如立方晶和六角晶。脂质液晶纳米分散体的制备方法可分为自上而下法和自下而上法,常用的脂质是单油酸甘油酯和植烷三醇。脂质液晶纳米粒可以有效包载不同性质的药物,实现难溶性药物的增溶、水溶性药物的缓释,保护药物不被体内环境破坏,同时具有稳定性高及适用于不同给药途径等优点,在缓控释递药系统中的应用愈发受到关注。目前,研究者们正致力于脂质液晶的功能化,优化其释放特性,如在系统中添加第三成分以使其具有外部刺激响应性。本文重点综述了缓控释脂质液晶纳米载体的类型及相关研究进展。Amphiphilic lipids can self-assemble under specific conditions to form various reverse liquid- crystalline phases, which can be dispersed in excess water to obtain nano-dispersions with different structures, such as cubosomes and hexosomes. These nanoparticles can effectively load drugs with characteristics of hydrophilic, lipophilic or amphiphilic, and are suitable for different routes of administration. Their high stability and excellent ability of solubilizing insoluble molecules and realizing sustained-release delivery of water-soluble drugs make them promising drug delivery systems. The preparation methods are generally divided into top-down method and bottom-up method, and the commonly used lipids are glyceryl monooleate and phytantriol. Dispersion of nanoparticles significantly enlarges the surface area, resulting in an increase in the diffusion rate of drugs from the matrices of the carriers, which makes them difficult to directly apply to sustained- and controlled-release systems. Therefore, researchers are working on optimizing their release characteristics by functionalization of the lipid liquid crystalline, such as adding a third component into the systems to make them response to external stimulations. This paper puts emphasis on the types and research advances of lipid liquid crystalline nanocarriers for sustained- and controlled-release.

关 键 词：脂质液晶 纳米载体 缓控释 两亲性脂质 环境响应性 综述 

分 类 号：R944.9[医药卫生—药剂学]