title: Influence of surfactants in self-microemulsifying formulations on enhancing oral bioavailability of oxyresveratrol: Studies in Caco-2 cells and in vivo.
abstract: Self-microemulsifying drug delivery systems (SMEDDS) containing two types (Tween80 and Labrasol) and two levels (low; 5% and high; 15%) of co-surfactants were formulated to evaluate the impact of surfactant phase on physical properties and oral absorption of oxyresveratrol (OXY). All formulations showed a very rapid release in the simulated gastric fluid (SGF) pH 1.2. After dilution with different media, the microemulsion droplet sizes of the Tween80-based (∼26 to 36 nm) were smaller than that of the Labrasol-based systems (∼34 to 45 nm). Both systems with high levels of surfactant increased the Caco-2 cells permeability of OXY compared to those with low levels of surfactant (1.4-1.7 folds) and the unformulated OXY (1.9-2.0 folds). It was of interest, that there was a reduction (4.4-5.3 folds) in the efflux transport of OXY from both systems compared to the unformulated OXY. The results were in good agreement with the in vivo absorption studies of such OXY-formulations in rats. Significantly greater values of Cmax and AUC(0-10h) (p<0.05) were obtained from the high levels of Tween80-based (F(r,0-10h) 786.32%) compared to those from the Labrasol-based system (F(r,0-10h) 218.32%). These finding indicate the importance of formulation variables such as type and quantity of surfactant in the SMEDDS to enhance oral drug bioavailability.
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: s.yaowaporn@gmail.com.
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. Electronic address: kamonthip.w@psu.ac.th.
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. Electronic address: Kittisak.L@chula.ac.th.
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. Electronic address: boonchoo.sr@chula.ac.th.
authors.forename: Boonchoo
authors.initials: B
authors.lastname: Sritularak
authors.affiliation: Department of Biomedical Sciences, Faculty of Medicine, Prince of Songkla University, Hat-Yai, Songkhla 90110, Thailand; The Excellent Research Laboratory of Cancer Molecular Biology, Prince of Songkla University, Hat-Yai, Songkhla 90110, Thailand. Electronic address: gpotchan@medicine.psu.ac.th.
authors.forename: Potchanapond
authors.initials: P
authors.lastname: Graidist
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; D001682:Biological Availability; D018938:Caco-2 Cells; D002626:Chemistry, Pharmaceutical; D004655:Emulsions / Q000008:administration & dosage / Q000737:chemistry* / Q000493:pharmacokinetics*; D006801:Humans; D008297:Male; D010936:Plant Extracts / Q000008:administration & dosage / Q000737:chemistry* / Q000493:pharmacokinetics*; D051381:Rats; D017208:Rats, Wistar; D013267:Stilbenes / Q000008:administration & dosage / Q000737:chemistry* / Q000493:pharmacokinetics*; D013501:Surface-Active Agents / Q000008:administration & dosage / Q000737:chemistry* / Q000493:pharmacokinetics*
chemical_list: D004655:Emulsions; D010936:Plant Extracts; D013267:Stilbenes; D013501:Surface-Active Agents; C034912:puag-haad
keywords: Caco-2 cells; Oral absorption; Oxyresveratrol; SMEDDS; Self-microemulsifying drug delivery system; Surfactants