Methylated β-cyclodextrin as P-gp modulators for deliverance of doxorubicin across an in vitro model of blood-brain barrier

被引：45
|
作者：
Tilloy, S
Monnaert, V
Fenart, L
Bricout, H
Cecchelli, R
Monflier, E
机构：
[1] Univ Artois, CNRS, FRE 2485, Lab Physicochim Interfaces & Applicat, F-62307 Lens, France
[2] Univ Artois, Fac Sci Jean Perrin, Blood Brain Barrier Lab, EA 2465, F-62307 Lens, France
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2006年 / 16卷 / 08期
关键词：
cyclodextrin; doxorubicin; P-glycoprotein; blood-brain barrier; cholesterol;
D O I：
10.1016/j.bmcl.2006.01.049
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Co-incubations of various beta-cyclodextrins and doxorubicin have been evaluated on an in vitro model of blood-brain barrier in order to increase the delivery of this P-gp substrate to the brain. Among these cyclodextrins used, the Rame-beta-cyclodextrin and Crysme-beta-cyclodextrin increased the transport by a factor of 2 and 3.7, respectively. This increase was attributed to the cholesterol extraction property of these cyclodextrins from brain capillary endothelial cells leading to a modulation of the P-gp activity. (C) 2006 Elsevier Ltd. All rights reserved.
引用
收藏
页码：2154 / 2157
页数：4
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