非离子表面活性剂在脑靶向传递系统中的研究进展

Advance in development of non-ionic surafctants in brain-targeted drug delivery systems

由于血脑屏障的存在,限制了很多药物脑靶向的使用及疗效。研究者们使用非离子表面活性剂与载体偶联,通过吸收血液中的载脂蛋白促进受体介导的内吞作用,以及抑制P-糖蛋白外排等机制,或者用非离子表面活性剂连接相应配体和单克隆抗体等方法,可以增加脑部对药物的摄取。本文综述了血脑屏障的结构特点,以及如何通过非离子表面活性剂的修饰使药物穿过血脑屏障,对实现脑靶向给药有重要意义。

Due to the existence of blood brain barrier（ BBB）,the therapeutic effects and distribution of many brain-targeted drugs are strictly regulated. Non-ionic surafctants-coated nanoparticles have therefore been used to increase the permeability of BBB as well as the specificity of drug targeting in the brain by diverse mechanisms which include absorbing apolipoprotein in plasma,facilitating endocytosis induced by receptor,and inhibiting P-glycoprotein efflux system on the blood brain barrier. On the other hand,specific ligands and monoclonal antibodies connecting to non-ionic surafctants can also increase the drug concentration in the brain. A large number of statistics showed that polysorbate 80 and poloxamer play an especially important role in brain-targeted drug delivery systems. In this paper,the structure of BBB and drug delivery across BBB by transporters modified by non-ionic surafctants are reviewed,with the aim to provide some guidance for the design of brain-targeted drug delivery systems.