Improved bioavailability of poorly water-soluble drug curcumin in cellulose acetate solid dispersion.
AAPS PharmSciTech
; 13(1): 159-66, 2012 Mar.
Article
em En
| MEDLINE
| ID: mdl-22173375
ABSTRACT
Curcumin (Cur), one of the most widely used natural active constituents with a great variety of beneficial biological and pharmacological activities, is a practically water-insoluble substance with a short biologic half-life. The aim of this study was to develop a sustained-release solid dispersion by employing water-insoluble carrier cellulose acetate for solubility enhancement, release control, and oral bioavailability improvement of Cur. Solid dispersions were characterized by solubility, in vitro drug release, Fourier transform infrared spectroscopy, X-ray diffractometry, and differential scanning calorimetry studies. The in vivo performance was assessed by a pharmacokinetic study. Solid-state characterization techniques revealed the amorphous nature of Cur in solid dispersions. Solubility/dissolution of Cur was enhanced in the formulations in comparison with pure drug. Sustained-release profiles of Cur from the solid dispersions were ideally controlled in vitro up to 12 h. The optimized formulation provided an improved pharmacokinetic parameter (C(max) = 187.03 ng/ml, t(max) = 1.95 h) in rats as compared with pure drug (C(max) = 87.06 ng/ml, t(max) = 0.66 h). The information from this study suggests that the developed solid dispersions successfully enhanced the solubility and sustained release of poorly water-soluble drug Cur, thus improving its oral bioavailability effectively.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Água
/
Celulose
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Curcumina
Limite:
Animals
Idioma:
En
Ano de publicação:
2012
Tipo de documento:
Article