Pharmaceutical Nanotechnology Tocol modified glycol chitosan for the oral delivery of poorly soluble drugs

The aim of this study was to develop tocol derivatives of chitosan able (i) to self-assemble in the gastroin-testinal tract and (ii) to enhance the solubility of poorly soluble drugs. Among the derivatives synthesized, tocopherol succinate glycol chitosan (GC-TOS) conjugates spontaneously formed mic...

Full description

Saved in:
Bibliographic Details
Published in:International journal of pharmaceutics 2012
Main Authors: Duhem, Nicolas, Riva, Raphael, Guillet, Pierre, Schumers, Jean-Marc, Jérome, Christine, Gohy, Jean-François, Préat, Véronique
Format: Article
Language:English
Subjects:
Chemical Sciences
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary:The aim of this study was to develop tocol derivatives of chitosan able (i) to self-assemble in the gastroin-testinal 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 ␮g 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.
ISSN:0378-5173
DOI:10.1016/j.ijpharm.2011.12.010