[en] The aim of this study was to develop tocol derivatives of chitosan able (i) to self-assemble in the gastrointestinal tract and (ii) to enhance the solubility of poorly soluble drugs. Among the derivatives synthesized, tocopherol succinate glycol chitosan (GC-TOS) conjugates spontaneously formed micelles in aqueous solution with a critical micelle concentration of 2 μg mL−1. AFM and TEM analysis showed that spherical micelles were formed. The GC-TOS increased water solubility of 2 model class II drugs. GC-TOS loading efficiency was 2.4% (w/w) for ketoconazole and 0.14% (w/w) for itraconazole, respectively. GC-TOS was non-cytotoxic at concentrations up to 10 mg mL−1. A 3.4-fold increase of the apparent permeation coefficient of ketoconazole across a Caco-2 cell monolayer was demonstrated. Tocol polymer conjugates may be promising vehicles for the oral delivery of poorly soluble drugs.
Research center :
Center for Education and Research on Macromolecules (CERM)
Disciplines :
Materials science & engineering Chemistry
Author, co-author :
Duhem, Nicolas; Université catholique de Louvain (UCL), Brussels > Louvain Drug Research Institute (LDRI) > Pharmaceutics and Drug Delivery
Rolland, Julien; Université catholique de Louvain (UCL) > Institute of Condensed Matter and Nanosciences > Bio and Soft Matter
Riva, Raphaël ; Université de Liège - ULiège > Department of Chemistry > Center for Education and Research on Macromolecules (CERM)
Guillet, Pierre; Université catholique de Louvain (UCL) > Institute of Condensed Matter and Nanosciences > Bio and Soft Matter
Schumers, Jean-Marc; Université catholique de Louvain (UCL) > Institute of Condensed Matter and Nanosciences > Bio and Soft Matter
Jérôme, Christine ; Université de Liège - ULiège > Department of Chemistry > Center for Education and Research on Macromolecules (CERM)
Gohy, Jean-François; Université catholique de Louvain (UCL) > Institute of Condensed Matter and Nanosciences > Bio and Soft Matter
Préat, Véronique; Université catholique de Louvain (UCL), Brussels > Louvain Drug Research Institute (LDRI) > Pharmaceutics and Drug Delivery
Language :
English
Title :
Tocol modified glycol chitosan for the oral delivery of poorly soluble drugs
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