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血脑屏障渗透模型PAMPA的构建及其应用

发表时间:2014-06-15  浏览量:2074  下载量:572
全部作者: 马林楠,刘晖,倪京满
作者单位: 兰州大学药学院
摘 要: 目的:建立血脑屏障体外模型——平行人工膜渗透模型(parallel artificial membrane permeation assay,PAMPA),并对系列小分子化合物进行评筛。方法:用牛脑磷脂(porcine polar brain lipid, PBL)的十二烷溶液在Multi Screen IP板上建立PAMPA模型,以实验室设计合成的氨基氧化吲哚类系列化合物为研究对象,高效液相色谱法(high performance liquid chromatography,HPLC)作为测定方法,计算血脑屏障渗透系数。结果:5 μL PBL/十二烷涂膜,25℃孵育16 h,控制助溶剂DMSO浓度小于5%,在此条件下,可形成稳定可靠的人工膜模型。结论:PAMPA模型作为早期预测药物通过被动扩散方式透过血脑屏障的体外模型是一个低成本、简便可靠的方法。
关 键 词: 药剂学;平行人工膜渗透模型;血脑屏障;模型构建
Title: Model establishment and application of PAMPA for blood-brain barrier
Author: MA Linnan, LIU Hui, NI Jingman
Organization: School of Pharmacy, Lanzhou University
Abstract: Objective: The aim of the study was to identify a model for the blood-brain barrier based on the use of the parallel artificial membrane permeation assay (PAMPA) model, and to predict the blood-brain barrier permeability of a set of test compounds. Methods: The filter membrane was coated with porcine polar brain lipid (PBL) in dodecane and effective permeability of the compounds was calculated by using high performance liquid chromatography (HPLC). Results: The filter membrane was coated with 5 μL PBL in dodecane, the concentration of DMSO was below 5%, and incubated for 16 h at 25℃ while the permeation occurred. On this condition, a steady and reliable artificial membrane assay was developed. Conclusion: The PAMPA has the advantages of predicting passive blood-brain barrier penetration with low cost and reproducibility.
Key words: pharmacy; parallel artificial membrane permeation assay; blood-brain barrier; model establishment
发表期数: 2014年6月第11期
引用格式: 马林楠,刘晖,倪京满. 血脑屏障渗透模型PAMPA的构建及其应用[J]. 中国科技论文在线精品论文,2014,7(11):1092-1096.
 
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