化学修饰提高药物跨膜递送效率研究进展

Advance in Research on Chemical Modification to Improve Intracellular Delivery of Drugs

药物分子穿透细胞膜进入胞内靶点是其发挥生物活性的先决条件。细胞膜作为阻止外源性有害物质侵入的防御性壁垒,使得生物大分子诊疗试剂的高效递送面临巨大挑战。通过对药物的化学修饰,基于修饰部件与细胞膜的相互作用来提高跨膜效率,是目前被证明行之有效并被广泛采用的方法。文章综述了目前通过化学改性提高药物跨膜效率的几种常用方法,旨在给新型高效药物递送体系的构建提供思路。

The cellular internalization of therapeutical drugs is a prerequisite for their biological activity.The efficient intracellular delivery of biomacromolecule drugs remains a long-standing challenge due to the impenetrability of cellular membrane which works as a defensive barrier to prevent the invasion of exogenous harmful substances.It is an efficient approach to improve the efficiency of intracellular delivery by chemical modification based on the interaction between modified components and cell membranes.Herein,we review several common strategies for intracellular delivery in order to provide some suggestions for the development of efficient drug delivery systems.