Department of Bioorganic & Pharmaceutical Chemistry, Faculty of Pharmacy, Al-Quds University, Jerusalem P.O. Box 20002, Palestine.
Molecules. 2018 May 28;23(6):1289. doi: 10.3390/molecules23061289.
The blood brain barrier (BBB) is a dynamic and functional structure which poses a vast challenge in the development of drugs acting on the central nervous system (CNS). While most substances are denied BBB crossing, selective penetration of substances mainly occurs through diffusion, carrier mediated transport, or receptor mediated transcytosis. Strategies in enhancing BBB penetration have been reviewed and summarized in accordance with their type of formulation. Highlights in monoclonal antibodies, peptide-vectors, nanoparticles, and simple prodrugs were included. Nanoparticles and simple prodrugs, for example, can be used for efficient BBB penetration through inhibition of efflux mechanisms, however, monoclonal antibodies are the most promising strategy in BBB penetration. Close follow-up of future development in this area should confirm our expectation.
血脑屏障（BBB）是一种动态而又具有功能性的结构，这给作用于中枢神经系统（CNS）的药物开发带来了巨大的挑战。大多数物质都不能穿透 BBB，而物质的选择性渗透主要通过扩散、载体介导的转运或受体介导的胞吞作用来实现。本文根据制剂类型对增强 BBB 穿透的策略进行了综述和总结。重点介绍了单克隆抗体、肽载体、纳米粒子和简单前药。例如，纳米粒子和简单前药可通过抑制外排机制来实现高效的 BBB 穿透，而单克隆抗体则是 BBB 穿透最有前途的策略。密切关注该领域的未来发展，应该能够证实我们的预期。
