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KMID : 0369820150450070633
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Jorunal of Korean Pharmaceutical Sciences
2015 Volume.45 No. 7 p.633 ~ p.640
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Enhanced oral bioavailability of naringenin administered in a mixed micelle formulation with Pluronic F127 and Tween 80 in rats
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Song Im-Sook
Cha Jin-Sun
Choi Min-Koo
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Abstract
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This study was aimed at developing a naringenin formulation to enhance its solubility and intestinal permeability and, thereby, overcome its low bioavailability. The naringenin-loaded mixed micelle formulation with a naringenin:Pluronic F127:Tween 80 ratio of 1:10:0.2 (w/w/w) was prepared using a thin-film hydration method. The solubility, size distribution, and cell viability were characterized. Subsequently, in vivo pharmacokinetic parameters of the naringenin-loaded mixed-micelle formulation were investigated in rats. The formulation increased the solubility of naringenin by 27-fold without a significant decrease in the viability of treated cells. The absolute bioavailability of naringenin dramatically increased from 4.1 to 26.9 % following per oral administration of naringenin-loaded mixed-micelle form. Absorption permeability of naringenin from the developed formulation increased by 1.7-fold compared to that of naringenin administered alone. In conclusion, the enhanced oral bioavailability of naringenin from the loaded mixed micelle formulation can be attributed to its increased solubility and intestinal permeation.
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KEYWORD
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Naringenin, Mixed micelle, Solubility, Permeability, Oral bioavailability
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