A versatile liposome/cyclodextrin supramolecular carrier for drug delivery through the blood-brain barrier

Cécile Machut-Binkowski Frédéric Hapiot 1 Roméo Cecchelli 2 Patrick Martin 3 Eric Monflier 4
1 LPCIA - Laboratoire de physico-chimie des interfaces et applications
2 LBHE - Laboratoire de Physiopathologie de la Barrière Hémato-Encéphalique
3 LGIPM - Laboratoire de Génie Industriel, de Production et de Maintenance
4 UCCS Artois - Unité de Catalyse et de Chimie du Solide - Site Artois
Abstract : For many commercial drugs, reaching the central nervous system in large amount without damaging the blood-brain-barrier (BBB) remains a challenging task. We present here a supramolecular strategy aiming at using a well-defined cyclodextrincoated liposomes as drug carrier and adamantoyl saccharides as BBB-interacting ligands. In this study, the liposome is constituted of n-alkyldimethylammoniumcyclodextrins incorporated in the lipid bilayer of a 3/7 cholesterol/dipalmitoylphosphatidylcholine mixture and the ligand is constituted of an adamantoylglucose molecule whose adamantoyl moiety can be included in the CD cavity. The whole supramolecular assembly has been characterized by light-scattering and 31P NMR measurements. Toxicity and permeability studies on an in vitro model of the BBB clearly demonstrated a 5-fold improved ability of the modified liposome to enter the BBB-endothelial cells compared to the non-coated liposome. Fluorescence labelling of these liposomes is also displayed with DiI as a fluorescent probe.
Keywords : Blood-brain-barrier Cyclodextrin Drug delivery In vitro model Liposome Saccharide Supramolecular chemistry
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Journal articles
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https://hal-univ-artois.archives-ouvertes.fr/hal-00546048
Contributor : Wilfried Déplanques <>
Submitted on : Monday, December 13, 2010 - 3:25:07 PM
Last modification on : Thursday, February 21, 2019 - 10:34:05 AM

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  • HAL Id : hal-00546048, version 1

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UNIV-ARTOIS | LGIPM | UNIV-LORRAINE | UCCS | INC-CNRS

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Cécile Machut-Binkowski, Frédéric Hapiot, Roméo Cecchelli, Patrick Martin, Eric Monflier. A versatile liposome/cyclodextrin supramolecular carrier for drug delivery through the blood-brain barrier. Journal of Inclusion Phenomena and Macrocyclic Chemistry, Springer Verlag, 2007, 57, p. 567-572. ⟨hal-00546048⟩

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