血脑屏障(Blood-brain barrier,BBB)的存在限制了血液中的大多数物质包括药物进入中枢神经系统(Central nervous system,CNS)。在新药研发的早期利用体外BBB模型评价药物的BBB通透性对于后续的动物和临床试验至关重要。本文主要综述了近年来BBB体外试验模型的研究进展及其在药物脑部转运方面的应用,为CNS新药研发、药动学和毒理学研究、脑靶向给药系统和临床治疗方案的发展提供新的思路和依据。
The blood-brain barrier( BBB) restricts the brain uptake of many substances including drugs,presenting a major challenge for the central nervous system( CNS) drug development. Thus,the development of in vitro BBB models is quiet essential to study the BBB permeability of CNS drugs in the early-stage of drug discovery,which can precede and complement animal and human studies. This article reviews the recent development of in vitro BBB models along with their applications in evaluating drug transport across BBB to provide new ideas and reference for the RD,pharmacokinetic and toxicological studies,development of brain-targeting drug delivery systems and clinical therapeutic protocols for CNS drugs.