中枢神经系统药物脑部递送体内评价方法

Evaluation of drug delivery to central nervous system in vivo

血脑屏障在保护中枢神经系统正常功能的同时也阻止了诊断和治疗药物的脑部递送。在新药研发过程中,评价中枢神经系统药物跨血脑屏障转运入脑的能力对于疾病诊疗非常关键。本文对近年来用于中枢神经系统药物入脑效率的主要体内评价方法进行了总结,为用于治疗中枢系统疾病的药物体内研究提供药动学和药效学的方法学依据。

The blood-brain barrier（ BBB） frustrates the diagnosis and therapeutic interventions by the same mechanisms that protect the central nervous system（ CNS） against intrusive chemicals. It is very important to assess the BBB permeability of drugs for CNS diseases in the stage of drug discovery. In this review,several methods and techniques in vivo for brain targeting assessment are discussed,so as to offer pharmacokinetic and pharmacodynamic evaluation methods to investigate drugs for CNS diseases treatment.