纳米药物载体的结构修饰实现内体逃逸-中国材料进展

文章信息/Info

Title:: Research Progress of Structural Modification of Drug Carrier to Achieve Endosome Escape

作者:: 李成龙1; 李荣烨1; 云鹏1; 张冠宏2; 郗来顺1; 王元斗1; 宿烽1; （1.青岛科技大学化工学院，山东青岛 266042）（2.胜利油田中心医院，山东东营，257000）

Author(s):: LI Chenglong1; LI Rongye1; YUN Peng1; ZHANG Guanhong2; XI Laishun1; WANG Yuandou1; SU Feng1; （1.College of Chemical Engineering, Qingdao University of Science and Technology, Qingdao 266042, China）（2.Shengli Oilfield Central Hospital, Dongying 257000, China）

Keywords:: drug carriers; endosome escape; protonation; photochemical internalization; structural modification

摘要:: 纳米药物载体因其良好的生物相容性、组织渗透性、无毒、易吸收等特性，得到广泛应用。药物载体进入靶向部位发挥作用需要以内吞方式进入细胞，在此过程中，内体的屏障作用是限制其发挥药效的重要因素。从逃逸机制出发，总结了逃逸剂通过质子化效应、膜融合或膜孔形成、膜破坏及屏蔽免疫等方式实现内体逃逸。综述了以聚合物材料、多肽、光化学试剂、pH敏感材料等为逃逸剂，对载体材料进行修饰，实现内体逃逸的方法，最后对载体内体逃逸的发展进行了展望。

Abstract:: Nanocarriers have been widely used for drug delivery because of their good biocompatibility, tissue permeability, nontoxicity, and easy absorption. The drug carrier enters the target site by cell endocytosis. During this process, the barrier function of the endosome is an important factor limiting the efficiency of drugs. This paper starts from the mechanism of endosome escape. The escape agents realize the endosomal escape by means of protonation effects, membrane fusing or membrane pore forming, membrane destructing, and immunity shielding. The modification of the carrier material by using the escape agents like polymer materials, peptides, photochemical reagents, and pHsensitive materials to achieve the escape are reviewed. Finally, the future development of the escape of the endosome is prospected.