title: Modification of oral absorption of oxyresveratrol using lipid based nanoparticles.
abstract: The aim of this study was to develop and assess nanostructured lipid carriers (NLC) compared to solid lipid nanoparticles (SLN) for improving the oral bioavailability of oxyresveratrol (OXY). The OXY formulated as SLN (OXY-SLN) and NLC (OXY-NLC) were prepared by a high shear homogenization technique. The optimized OXY-NLC (NLC3) produced smaller nanoparticle sizes (96±0.9nm) than that of the OXY-SLN (108±0.3nm) with a homogeneous size distribution and a high zeta potential. The spherical NLC had a significantly higher efficiency for OXY entrapment (89±0.1%) and a better stability than the SLN after storage for 12 months at 4±2°C according to parameters such as smaller particles, greater zeta potential and a higher loading capacity (p<0.05). Differential scanning calorimetry (DSC) showed a less ordered crystalline structure of NLC than SLN. The accumulated drug in an amorphous state in the NLC was also confirmed by powder X-ray diffraction (PXRD). The in vitro release profiles of the OXY-NLC showed a more sustained release compared to the SLN and unformulated OXY. The in vivo pharmacokinetic profiles implied enterohepatic recycling of OXY in the Wistar rat. Meanwhile, the oral absorption pattern of OXY was modified by both types of lipid nanoparticles. The SLN and NLC increased the relative bioavailability of OXY to 125% and 177%, respectively, compared with unformulated OXY. These findings indicated that NLC could be used as a potential carrier to improve the oral bioavailability of OXY.
authors.affiliation: Department of Pharmaceutical Technology, Faculty of Pharmaceutical Sciences, Prince of Songkla University, Hat-Yai, Songkhla 90112, Thailand; Phytomedicine and Pharmaceutical Biotechnology Excellence Research Center, Faculty of Pharmaceutical Sciences, Prince of Songkla University, Hat-Yai, Songkhla 90112, Thailand.
authors.forename: Yaowaporn
authors.initials: Y
authors.lastname: Sangsen
authors.affiliation: Phytomedicine and Pharmaceutical Biotechnology Excellence Research Center, Faculty of Pharmaceutical Sciences, Prince of Songkla University, Hat-Yai, Songkhla 90112, Thailand; Department of Clinical Pharmacy, Faculty of Pharmaceutical Sciences, Prince of Songkla University, Hat-Yai, Songkhla 90112, Thailand.
authors.forename: Kamonthip
authors.initials: K
authors.lastname: Wiwattanawongsa
authors.affiliation: Department of Pharmacognosy and Pharmaceutical Botany, Faculty of Pharmaceutical Sciences, Chulalongkorn University, Bangkok 10330, Thailand.
authors.forename: Kittisak
authors.initials: K
authors.lastname: Likhitwitayawuid
authors.affiliation: Department of Pharmacognosy and Pharmaceutical Botany, Faculty of Pharmaceutical Sciences, Chulalongkorn University, Bangkok 10330, Thailand.
authors.forename: Boonchoo
authors.initials: B
authors.lastname: Sritularak
authors.affiliation: Department of Pharmaceutical Technology, Faculty of Pharmaceutical Sciences, Prince of Songkla University, Hat-Yai, Songkhla 90112, Thailand; Phytomedicine and Pharmaceutical Biotechnology Excellence Research Center, Faculty of Pharmaceutical Sciences, Prince of Songkla University, Hat-Yai, Songkhla 90112, Thailand. Electronic address: ruedeekorn.w@psu.ac.th.
authors.forename: Ruedeekorn
authors.initials: R
authors.lastname: Wiwattanapatapee
mesh_terms: D000284:Administration, Oral; D000818:Animals; D002152:Calorimetry, Differential Scanning; D004337:Drug Carriers / Q000737:chemistry; D004553:Electric Conductivity; D007408:Intestinal Absorption; D007700:Kinetics; D008055:Lipids / Q000737:chemistry*; D008297:Male; D046529:Microscopy, Electron, Transmission; D053758:Nanoparticles / Q000737:chemistry* / Q000648:ultrastructure; D010316:Particle Size; D010936:Plant Extracts / Q000008:administration & dosage / Q000493:pharmacokinetics*; D017208:Rats, Wistar; D055672:Static Electricity; D013267:Stilbenes / Q000008:administration & dosage / Q000493:pharmacokinetics*; D014961:X-Ray Diffraction
chemical_list: D004337:Drug Carriers; D008055:Lipids; D010936:Plant Extracts; D013267:Stilbenes; C034912:puag-haad
keywords: Nanostructured lipid carriers; Oral absorption; Oxyresveratrol; Solid lipid nanoparticles