Fan Weiwei, Xia Dengning, Zhu Quanlei, Hu Lei, Gan Yong
Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China.
Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China; Nano Science and Technology Institute, University of Science and Technology of China, Anhui 230026, China.
Drug Discov Today. 2016 May;21(5):856-63. doi: 10.1016/j.drudis.2016.04.007. Epub 2016 Apr 14.
The intestinal epithelium is the main barrier restricting the oral delivery of low-permeability drugs. Over recent years, numerous nanocarriers have been designed to improve the efficiency of oral drug delivery. However, the intracellular processes determining the transport of nanocarriers across the intestinal epithelium remain elusive, and only limited enhancement of the oral bioavailability of drugs has been achieved. Here, we review the processes involved in nanocarrier trafficking across the intestinal epithelium, including apical endocytosis, intracellular transport, and basolateral exocytosis. Understanding the complex intracellular processes of nanocarrier trafficking is particularly essential for the rational design of oral drug delivery systems.
肠上皮是限制低渗透性药物口服给药的主要屏障。近年来,人们设计了许多纳米载体来提高口服给药的效率。然而,决定纳米载体跨肠上皮转运的细胞内过程仍不清楚,药物口服生物利用度仅得到有限提高。在此,我们综述了纳米载体跨肠上皮运输所涉及的过程,包括顶端内吞作用、细胞内运输和基底外侧胞吐作用。了解纳米载体运输复杂的细胞内过程对于合理设计口服给药系统尤为重要。