Preparation and in vitro and in vivo evaluation of quercetin-loaded mixed micelles for oral delivery |
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| Authors: | Zhen Lu Cuiping Bu Weicheng Hu Hui Zhang Mengrui Liu Meiqi Lu |
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| Institution: | 1. Department of Pharmacy, Taian Rongjun Hospital of Shandong Province, Taian, China;2. Jiangsu Key Laboratory for Eco-Agricultural Biotechnology around Hongze Lake, Huaiyin Normal University, Huai’an, China;3. Department of Pharmaceutics, College of Pharmacy, Shandong University, Jinan, China;4. The First Clinical Medical College, Shandong University of Traditional Chinese Medicine, Jinan, China |
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| Abstract: | 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 Cmax and AUC0–24 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. |
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| Keywords: | Mixed micelles quercetin sodium taurocholate Pluronic P123 |
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