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- Title
Preparation and in vitro and in vivo evaluation of quercetin-loaded mixed micelles for oral delivery.
- Authors
Lu, Zhen; Bu, Cuiping; Hu, Weicheng; Zhang, Hui; Liu, Mengrui; Lu, Meiqi; Zhai, Guangxi
- 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 determinedin vitroin simulated gastric fluid and intestinal fluid. Pharmacokinetic evaluation showed theCmaxand AUC0–24were 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. Schematic illustration of QT-loaded mixed micelles. ST, P123 and QT were dissolved in EtOH, then evaporated to obtain thin film, followed by hydration to form a uniform system.
- Subjects
BIOFLAVONOIDS; FLAVONOIDS
- Publication
Bioscience, Biotechnology & Biochemistry, 2018, Vol 82, Issue 2, p238
- ISSN
0916-8451
- Publication type
Article
- DOI
10.1080/09168451.2017.1419852