脂质体药物传递系统的50年发展历程概述

Summary on liposomes for drug delivery in 50 years development course

目的回顾脂质体50年发展过程中的重大突破及创新,并对其在药物传递系统中的卓越贡献进行综述。方法查阅国内外相关文献99篇,从发展的角度对其进行归纳、分析和总结。结果50年的技术发展与创新促进脂质体不断完善,从传统脂质体到长循环脂质体、从被动靶向到主动靶向、从小分子治疗到基因转染,使其作为一种新型载体系统在临床应用中发挥着越来越重要的作用。近些年研究发现的"加速血液清除"(accelerated blood clearance,ABC)现象极大地限制了PEG化脂质体制剂的临床应用,由此而提出减弱或消除此现象的方法也引起了人们的广泛关注。结论脂质体作为一种纳米载体,在不断发展与完善的同时,也为临床治疗提供了一种新的选择,并将在药物传递领域具有十分广阔的应用前景。

Objective To review the major breakthroughs and innovations of liposomes during the 50 years＇ development and summarize its outstanding contributions in drug delivery systems. Methods Referencing 99 domestic and overseas literatures, then induce, analyze and conclude the contributions of liposomes with the developing perspective. Results The technology development and innovation of liposomes in 50 years perfec- ted liposomes from traditional to long-circulating liposomes, from passive to active targeting, from small mo- lecular therapy to the gene transfection, which make liposomes as a new carrier system play a increasingly important role in clinic application. In recent years, the study found that accelerated blood clearance （ABC phenomenon） greatly restricted the clinical application of liposome preparations, thereby the methods to de- crease or eliminate the ABC phenomenon has attracted widespread attention. Conclusions With developing and improving continually, liposomes as a kind of nanoparticle systems, could provide a new way for clinical treatment and will have a very broad application prospects in the field of drug delivery.