期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 16, 期 8, 页码 2154-2157出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2006.01.049
关键词
cyclodextrin; doxorubicin; P-glycoprotein; blood-brain barrier; cholesterol
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.
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