泊洛沙姆是一种具有药理活性的多功能药用辅料,在药剂学中应用广泛。近年来,研究发现泊洛沙姆可以通过多种作用机制帮助药物穿越血脑屏障,抑制血脑屏障上的P-糖蛋白、多药耐药相关蛋白等外排泵系统;吸附血浆中的不同载脂蛋白后,通过与血脑屏障上相应受体的结合,使泊洛沙姆包被的纳米粒主动转运入脑;连接各种配体及单克隆抗体等导向性分子,使其通过受体介导的转运进入脑部。本文综述了泊洛沙姆在促进药物穿越血脑屏障的重要作用,对设计脑靶向药物传递系统具有重要意义。
Poloxamers are found generally in pharmaceutical field. In to be an efficient adjuvant with multiple effects and are applied recent years, it is investigated that poloxamers can increase the permeability of a broad spectrum of drugs through blood-brain barrier (BBB) by means of manifold mechanisms included: (1) inhibiting P-glycoprotein and muhidrug-resistance associated protein efflux systems on BBB ; (2) adsorbing different apolipoproteins in plasma on the surface of poloxamer-coated nanoparticles, which could interact with BBB through different receptors and mechanisms; (3) connecting to specific ligands and monoclonal antibodies to cross the BBB via specific endogenous transporters localized within the brain capillary endothelium. Significant roles of poloxamer in drug transport across BBB are considered in this review which provides for important guidance to the design of brain-targeted drug delivery system.