Improved solubility and oral bioavailability ofApigeninvia Soluplus®/Pluronic F127binary mixed micelles system.

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Improved solubility and oral bioavailability ofApigeninvia Soluplus®/Pluronic F127binary mixed micelles system.

Drug Dev Ind Pharm. 2017 Mar 30;:1-14

Authors: Zhang Z, Cui C, Wei F, Lv H

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.

PMID: 28358225 [PubMed - as supplied by publisher]

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