EPR作用及其在抗肿瘤大分子药物研究中的应用  

EPR effect and its application in research and development of anticancer macromolecular drugs

作　　者：郝爱军[1] 张宁[2] 郭兴家[2] 张相军[2] 

机构地区：[1]辽宁大学药学院,沈阳110036 [2]辽宁大学化学院,沈阳110036

出　　处：《中国新药杂志》2012年第21期2516-2520,共5页Chinese Journal of New Drugs

基　　金：辽宁省自然科学基金项目(20102087)

摘　　要：研究表明肿瘤或炎症附近组织的渗透性比正常组织大,大分子物质较易进入并积聚到肿瘤细胞附近,实现肿瘤的被动靶向。这种作用被称为高通透性和滞留效应,即EPR效应。EPR效应的发现在药学研究领域具有重要意义。EPR作用在靶向药物设计和开发中越来越受到重视,基于EPR靶向作用机理,近年来陆续研究和开发了许多高分子药物,其中很多已经上市。本文主要综述了有关EPR效应的机理、影响因素和基于EPR效应的靶向药物设计原理,探讨了EPR效应在抗癌药物靶向传递方面的应用。Many studies have demonstrated that the tissues near the tumors or inflammation exhibit higher permeability than normal tissues.So it will be easier for macromolecules to enter and accumulate in the tumors to achieve passive tumor targeting.This effect is called Enhanced Permeability and Retention effect,i.e.EPR effect.The demonstration of EPR effect is very important in the field of drug design and development.Recently,EPR effect has attracted more and more attentions in the field of targeted drug design and development.Many macromolecular drug based on EPR effect have come into market.There are more and more macromolecular drugs waiting for evaluation.This paper is aimed to review the mechanism of EPR effect and its application in anticancer drug design.The application of EPR effect in anticancer drugs targeting delivery systems is also discussed.

关 键 词：EPR效应 大分子药物 肿瘤靶向 

分 类 号：R943[医药卫生—药剂学] R979.1[医药卫生—药学]