title: Chitosan microparticles for oral bioavailability improvement of the hydrophobic drug curcumin.
abstract: 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.
authors: School of Pharmaceutical Science and Technology, Tianjin University, Tianjin, China.
authors: Shuxin
authors: S
authors: Wan
authors: Yingqian
authors: Y
authors: Sun
authors: Li
authors: L
authors: Sun
authors: Fengping
authors: F
authors: Tan
mesh_terms: D000818:Animals; D000975:Antioxidants / Q000008:administration & dosage* / Q000493:pharmacokinetics*; D001682:Biological Availability; D002586:Cesium / Q000737:chemistry; D048271:Chitosan / Q000737:chemistry*; D002851:Chromatography, High Pressure Liquid; D003432:Cross-Linking Reagents; D003474:Curcumin / Q000008:administration & dosage* / Q000493:pharmacokinetics*; D004339:Drug Compounding; D004563:Electrochemistry; D005079:Excipients; D057927:Hydrophobic and Hydrophilic Interactions; D008297:Male; D008855:Microscopy, Electron, Scanning; D053758:Nanoparticles; D010316:Particle Size; D011122:Polyphosphates; D051381:Rats; D017208:Rats, Wistar
chemical_list: D000975:Antioxidants; D003432:Cross-Linking Reagents; D005079:Excipients; D011122:Polyphosphates; D002586:Cesium; D048271:Chitosan; D003474:Curcumin; C005692:triphosphoric acid