Tocol modified glycol chitosan for the oral delivery of poorly soluble drugs.
Int J Pharm
; 423(2): 452-60, 2012 Feb 28.
Article
em En
| MEDLINE
| ID: mdl-22212463
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.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Portadores de Fármacos
/
Itraconazol
/
Tocoferóis
/
Quitosana
/
Cetoconazol
Limite:
Humans
Idioma:
En
Ano de publicação:
2012
Tipo de documento:
Article