Key Laboratory of Drug-Targeting and Drug Delivery System of the Education Ministry, Sichuan Engineering Laboratory for Plant-Sourced Drug and Sichuan Research Center for Drug Precision Industrial Technology, West China School of Pharmacy, Sichuan University, Chengdu, 610064, P. R. China.
Chem Commun (Camb). 2021 Sep 6;57(71):8842-8855. doi: 10.1039/d1cc02940a.
Central nervous system (CNS) disease is one of the most notorious arch-criminals of human health across the world. Although considerable efforts have been devoted to promote the development of CNS drugs, ideal therapeutical effects are yet far from enough. The blood-brain barrier remains a major player that impedes the full potential of CNS therapeutical agents as it blocks the entry of CNS drugs into the brain. The past few decades have witnessed the upspring of prodrug strategies as a promising method to accelerate CNS drug development. The prodrug strategy with the ability to overcome the formidable blood-brain barrier enhances the delivery to the brain and hence improves the effects of the CNS therapeutics. In this Feature Article, we summarize the reported barriers and strategies for CNS therapeutics and spotlight prodrug design strategies to improve the efficiency of crossing the blood-brain barrier.
中枢神经系统（CNS）疾病是全球人类健康最臭名昭著的罪魁祸首之一。尽管人们为促进中枢神经系统药物的发展做出了相当大的努力，但理想的治疗效果仍远远不够。血脑屏障仍然是一个主要的障碍，它阻止了中枢神经系统治疗药物的全部潜力，因为它阻止了中枢神经系统药物进入大脑。在过去的几十年里，前药策略作为一种有前途的方法来加速中枢神经系统药物的发展而兴起。具有克服强大血脑屏障能力的前药策略可以增强向大脑的递送，从而提高中枢神经系统治疗药物的效果。在这篇专题文章中，我们总结了报告的中枢神经系统治疗的障碍和策略，并重点介绍了前药设计策略，以提高穿过血脑屏障的效率。
