title: Improved solubility and oral bioavailability of apigenin via Soluplus/Pluronic F127 binary mixed micelles system.
abstract: The aim of this study was to develop a novel mix micelles system composing of two biocompatible copolymers of Soluplus®and Pluronic F127 to improve the solubility, oral bioavailability of insoluble drug apigenin (AP) as model drug. The AP-loaded mixed micelles (AP-M) were prepared by ethanol thin-film hydration method. The formed optimal formulation of AP-M were provided with small size (178.5 nm) and spherical shape at ratio of 4:1 (Soluplus®:Pluronic F127), as well as increasing solubility of to 5.61 mg/mL in water which was about 3442-fold compared to that of free AP. The entrapment efficiency and drug loading of AP-M were 95.72 and 5.32%, respectively, and a sustained release of AP-M was obtained as in vitro release study indicated. Transcellular transport study showed that the cell uptake of AP was increased in Caco-2 cell transport models. The oral bioavailability of AP-M was 4.03-fold of free AP in SD rats, indicating the mixed micelles of Soluplus®and Pluronic F127 is an industrially feasible drug delivery system to promote insoluble drug oral absorption in the gastrointestinal tract.
authors.affiliation: a Hospital of Integrated Traditional Chinese and Western Medicine Affiliated to Nanjing University of Chinese Medicine , Nanjing , PR China.|b Jiangsu Province Academy of Traditional Chinese Medicine , Nanjing , PR China.
authors.forename: Zhenhai
authors.initials: Z
authors.lastname: Zhang
authors.affiliation: c Department of Pharmaceutics, State Key Laboratory of Natural Medicines , China Pharmaceutical University , Nanjing , PR China.
authors.forename: Changchang
authors.initials: C
authors.lastname: Cui
authors.affiliation: a Hospital of Integrated Traditional Chinese and Western Medicine Affiliated to Nanjing University of Chinese Medicine , Nanjing , PR China.|b Jiangsu Province Academy of Traditional Chinese Medicine , Nanjing , PR China.
authors.forename: Fang
authors.initials: F
authors.lastname: Wei
authors.affiliation: c Department of Pharmaceutics, State Key Laboratory of Natural Medicines , China Pharmaceutical University , Nanjing , PR China.
authors.forename: Huixia
authors.initials: H
authors.lastname: Lv
mesh_terms: D000284:Administration, Oral; D000818:Animals; D047310:Apigenin / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics*; D001682:Biological Availability; D018938:Caco-2 Cells; D045744:Cell Line, Tumor; D016503:Drug Delivery Systems / Q000379:methods*; D006801:Humans; D008823:Micelles; D010316:Particle Size; D020442:Poloxamer / Q000737:chemistry* / Q000493:pharmacokinetics*; D011092:Polyethylene Glycols / Q000008:administration & dosage* / Q000737:chemistry; D011145:Polyvinyls / Q000008:administration & dosage* / Q000737:chemistry; D051381:Rats; D017207:Rats, Sprague-Dawley; D012995:Solubility
chemical_list: D008823:Micelles; D011145:Polyvinyls; C572167:polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer; D020442:Poloxamer; D011092:Polyethylene Glycols; D047310:Apigenin
keywords: Caco-2; Mix micelles system; Pluronic F127; Soluplus; apigenin; oral bioavailability