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血脑屏障(BBB)主要由脑毛细血管内皮细胞构成,其阻止98%小分子和几乎全部大分子化合物入脑,是制约脑药发展的重要因素.目前将药物递送入脑的主要途径为神经外科学、药化和生理学途径,后者利用脑毛细血管内皮细胞膜受体介导的跨细胞系统(RMT)为载体携载药物经主动转运入脑.基于RMT可构建促进药物入脑的载药平台,该文重点介绍该平台的研究思路、方法技术和应用前景等方面的最新研究进展.“,”The blood-brain barrier(BBB) is formed by the brain capillary endothelium and excludes from the brain approximately 100% of large-molecule neurotherapeutics and more than 98% of all small-molecule drugs.There are three routines to increase drug transport into brain,ie,neurosurgical,pharmaceutical chemical,and physiological ways and the later is most hopeful.The receptor-mediated transcytosis system on the brain capillary endothelium could be used as multifunctional vectors for drug active transport into brain.This provides the platform for CNS drug delivery programs.