脑部靶向给药的关键是使药物透过血脑屏障,提高药物的生物利用度。血脑屏障内皮细膜上的各种受体及转运体常用来作为非侵入式给药的靶点。本综述详细介绍了各种受体介导转运体系在脑部靶向给药中的应用。
本课题主要由房飞硕士完成,相关研究已经发表在Materials Science and Engineering C
http://dx.doi.org/10.1016/j.msec.2017.02.056
Non-invasive Approaches for Drug Delivery to the Brain Based on the Receptor Mediated Transport
Fei Fang, Dan Zou, Wei Wang, Ying Yin, Tieying Yin, Shilei Hao, Bochu Wang, Guixue Wang, Yazhou Wang*

The blood brain barrier (BBB) is a physical and biochemical barrier that prevents entry of toxic compounds into brain for preservinghomeostasis. However, the BBB also strictly limits influx of most therapeutic agents into the brain. One promising method for overcoming this problem to deliver drugs is receptor mediated transport (RMT) system, which employs the vesicular trafficking machinery to transport substrates across the BBB endothelium in a noninvasive manner. The conjugates of drug or drug-loaded vector linked with appropriate ligands specifically binds to the endogenous targeting receptor on the surface of the endothelial cells. Then drugs could enter the cell body by means of transcytosis and eventual releasing into the brain parenchyma. Over the past 20 years, there have been significant developments of RMT targeting strategies. Here, we will review the recent advance of various promising RMT systems and discuss the capability of these approaches for drug delivery to the brain.