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

Sébastien Tilloy 1 Véronique Monnaert 2 Laurence Fenart 2 Hervé Bricout 1 Roméo Cecchelli 2 Eric Monflier 3
1 Laboratoire de Physico-Chimie des Interfaces et Applications
2 LBHE - Laboratoire de Physiopathologie de la Barrière Hémato-Encéphalique
3 UCCS Artois - Unité de Catalyse et de Chimie du Solide - Site Artois
Abstract : Co-incubations of various β-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-β-cyclodextrin and Crysme-β-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.
Keywords : Cyclodextrin Doxorubicin P-glycoprotein Blood-brain barrier Cholesterol
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Journal articles
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https://hal-univ-artois.archives-ouvertes.fr/hal-00543357
Contributor : Wilfried Déplanques <>
Submitted on : Monday, December 6, 2010 - 1:35:53 PM
Last modification on : Thursday, February 21, 2019 - 10:34:05 AM

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Sébastien Tilloy, Véronique Monnaert, Laurence Fenart, Hervé Bricout, Roméo Cecchelli, et al.. Methylated β-cyclodextrin as P-gp modulators for deliverance of doxorubicin across an in vitro model of blood-brain barrier. Bioorganic and Medicinal Chemistry Letters, Elsevier, 2006, 16, p. 2154-2157. ⟨hal-00543357⟩

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