文章信息/Info

Title:

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

作者:

李成龍1; 李榮燁1; 云鵬1; 張冠宏2; 郗來(lái)順1; 王元斗1; 宿烽1

（1.青島科技大學(xué)化工學(xué)院，山東 青島 266042）（2.勝利油田中心醫(yī)院，山東 東營(yíng)，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）

關(guān)鍵詞:

藥物載體; 內(nèi)體逃逸; 質(zhì)子化; 光化學(xué)內(nèi)化; 結(jié)構(gòu)修飾

Keywords:

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

DOI:

10.7502/j.issn.1674-3962.2019.03.09

文獻(xiàn)標(biāo)志碼:

A

摘要:

納米藥物載體因其良好的生物相容性、組織滲透性、無(wú)毒、易吸收等特性，得到廣泛應(yīng)用。藥物載體進(jìn)入靶向部位發(fā)揮作用需要以內(nèi)吞方式進(jìn)入細(xì)胞，在此過(guò)程中，內(nèi)體的屏障作用是限制其發(fā)揮藥效的重要因素。從逃逸機(jī)制出發(fā)，總結(jié)了逃逸劑通過(guò)質(zhì)子化效應(yīng)、膜融合或膜孔形成、膜破壞及屏蔽免疫等方式實(shí)現(xiàn)內(nèi)體逃逸。綜述了以聚合物材料、多肽、光化學(xué)試劑、pH敏感材料等為逃逸劑，對(duì)載體材料進(jìn)行修飾，實(shí)現(xiàn)內(nèi)體逃逸的方法，最后對(duì)載體內(nèi)體逃逸的發(fā)展進(jìn)行了展望。

Abstract:

Nanocarriers have been widely used for drug delivery because of their good biocompatibility, tissue permeability, non�瞭oxicity, 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�瞫ensitive materials to achieve the escape are reviewed. Finally, the future development of the escape of the endosome is prospected.