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

页码：2154 / 2157

页数：4

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