Tocol modified glycol chitosan for the oral delivery of poorly soluble drugs
(2012) International Journal of Pharmaceutics — Vol. 423, n° 2, p. 452-460 (2012)
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- Abstract
- 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.
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Citations
Duhem, N., Rolland, J., Riva, R., Guillet, P., Schumers, J.-M., Jérome, C., Gohy, J.-F., & Préat, V. (2012). Tocol modified glycol chitosan for the oral delivery of poorly soluble drugs. International Journal of Pharmaceutics, 423(2), 452-460. https://doi.org/10.1016/j.ijpharm.2011.12.010 (Original work published 2012)