Improved solubility and oral bioavailability of apigenin via Soluplus/Pluronic F127 binary mixed micelles system |
| |
| Authors: | Zhenhai Zhang Changchang Cui Fang Wei Huixia Lv |
| |
| Affiliation: | 1. Hospital of Integrated Traditional Chinese and Western Medicine Affiliated to Nanjing University of Chinese Medicine, Nanjing, PR China;2. Jiangsu Province Academy of Traditional Chinese Medicine, Nanjing, PR China;3. Department of Pharmaceutics, State Key Laboratory of Natural Medicines, China Pharmaceutical University, Nanjing, PR China |
| |
| 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. |
| |
| Keywords: | Mix micelles system Soluplus Pluronic F127 apigenin oral bioavailability Caco-2 |
|
|
