Lu Zhen, Bu Cuiping, Hu Weicheng, Zhang Hui, Liu Mengrui, Lu Meiqi, Zhai Guangxi
a Department of Pharmacy , Taian Rongjun Hospital of Shandong Province , Taian , China.
b Jiangsu Key Laboratory for Eco-Agricultural Biotechnology around Hongze Lake , Huaiyin Normal University , Huai'an , China.
Biosci Biotechnol Biochem. 2018 Feb;82(2):238-246. doi: 10.1080/09168451.2017.1419852. Epub 2018 Jan 12.
Quercetin (QT) is a plant polyphenol with various pharmacological properties. However, the low water solubility limits its therapeutic efficacy. In the present study, QT-loaded sodium taurocholate-Pluronic P123 (QT-loaded ST/P123) mixed micelles were developed and characterized, and the effect of the formulation on improving the water solubility of QT was investigated. QT-loaded ST/P123 mixed micelles were prepared by thin film hydration-direct dissolution and optimized by uniform design. The optimal formulation possessed high drug loading (12.6%) and entrapment efficiency (95.9%) in small (16.20 nm) spherically-shaped micelles. A low critical micelle concentration indicated that the micelles were stable, and they showed a sustained release pattern, as determined in vitro in simulated gastric fluid and intestinal fluid. Pharmacokinetic evaluation showed the C and AUC were 1.8-fold and 1.6-fold higher than the QT suspension. The present results indicate that QT-loaded ST/P123 micelles are potential candidates to improve the solubility and oral bioavailability of QT.
槲皮素（QT）是一种具有多种药理特性的植物多酚。然而，其低水溶性限制了它的治疗效果。在本研究中，制备并表征了载槲皮素的牛磺胆酸钠-普朗尼克P123（载QT的ST/P123）混合胶束，并研究了该制剂对提高QT水溶性的作用。通过薄膜水化-直接溶解法制备载QT的ST/P123混合胶束，并采用均匀设计法进行优化。最佳制剂在小尺寸（16.20纳米）球形胶束中具有高载药量（12.6%）和包封率（95.9%）。低临界胶束浓度表明胶束稳定，并且在模拟胃液和肠液中体外测定显示它们呈现缓释模式。药代动力学评估表明，Cmax和AUC比QT混悬液分别高1.8倍和1.6倍。目前的结果表明，载QT的ST/P123胶束是提高QT溶解度和口服生物利用度的潜在候选物。
