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如何使药物有效地穿越血脑屏障并发挥药效,是治疗中枢神经系统疾病的一大难题。通过结构修饰,可以改善小分子药物的理化性质,使其通过被动扩散的方式到达脑部;另外,可将药物修饰成能借助载体或受体介导的转运系统运输的结构,经由载/受体转运进入脑部。这两种手段是目前常用的改善药物血脑屏障通透性的化学方法。本文简要介绍了药物传送到脑部的主要途径,并重点阐述基于传送途径对小分子药物利用化学手段进行结构修饰以改善药物血脑屏障通透性的方法。
How to effectively cross the blood-brain barrier and exert its efficacy is a major challenge in the treatment of central nervous system diseases. Through the structural modification, the physicochemical properties of the small molecule drug can be improved and can reach the brain through passive diffusion. In addition, the drug can be modified into a structure that can be transported by the carrier or the receptor-mediated transport system, Body transport into the brain. These two methods are currently used to improve the chemical permeability of the blood-brain barrier of the chemical method. This article briefly introduces the main routes of drug delivery to the brain and focuses on the methods of chemical modification of small molecule drugs based on the delivery route to improve the permeability of the blood-brain barrier of drugs.