title: Improved bioavailability of poorly water-soluble drug curcumin in cellulose acetate solid dispersion.
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.
authors.affiliation: Tianjin Key Laboratory of Modern Drug Delivery and High-Efficiency, School of Pharmaceutical Science and Technology, Tianjin University, People's Republic of China.
authors.forename: Shuxin
authors.initials: S
authors.lastname: Wan
authors.forename: Yingqian
authors.initials: Y
authors.lastname: Sun
authors.forename: Xiuxiang
authors.initials: X
authors.lastname: Qi
authors.forename: Fengping
authors.initials: F
authors.lastname: Tan
mesh_terms: D000818:Animals; D001682:Biological Availability; D002482:Cellulose / Q000031:analogs & derivatives* / Q000737:chemistry / Q000493:pharmacokinetics; D003474:Curcumin / Q000737:chemistry / Q000493:pharmacokinetics*; D008297:Male; D051381:Rats; D017208:Rats, Wistar; D012995:Solubility; D014867:Water / Q000737:chemistry / Q000378:metabolism*; D014961:X-Ray Diffraction
chemical_list: D014867:Water; C005062:acetylcellulose; D002482:Cellulose; D003474:Curcumin