Chitosan microparticles for oral bioavailability improvement of the hydrophobic drug curcumin.

The aim of this study was to assess the feasibility of microparticles for dissolution enhancement and oral bioavailability of curcumin (Cur). Microparticles were prepared by the ionic crosslinking interaction with the use of tripolyphosphate (TPP) and chitosan (Cs). The physicochemical characteristics of microparticles were investigated. The in vivo performance was assessed by a pharmacokinetic study. The microparticles had an average diameter of 58.50 microm. Acceptable drug loading and encapsulation efficiency of microparticles were obtained to be 33.5% and 85.2%, respectively. Dissolution of Cur enhanced in the microparticles in comparison with pure drug. Drug release profile of Cur from microparticles fitted the first-order model. Microparticles provided improved pharmacokinetic parameters (Cmax 270.24 ng/ml, T(max) 1.30 h) in rats as compared with pure drug (C(max) 87.06 nglml, Tmax 0.66 h). The AUC value of microparticles was 8.4 fold that of the pure drug. The information from this study suggests that the developed microparticles successfully enhanced dissolution of the poorly water-soluble drug Cur, and eventually, improved its oral bioavailability effectively.

Improved bioavailability of poorly water-soluble drug curcumin in cellulose acetate solid dispersion.

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.