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利用负载芹菜素的 W/O/W 乳液制剂提高口服生物利用度:体外和体内评价。

Enhancing oral bioavailability using preparations of apigenin-loaded W/O/W emulsions: In vitro and in vivo evaluations.

机构信息

Korea Food Research Institute, 1201-62 Anyangpangyo-Ro, Baekhyun-Dong, Bundang-Ku, Songnam-Si, Kyunggi-Do 463-746, Republic of Korea.

Korea Food Research Institute, 1201-62 Anyangpangyo-Ro, Baekhyun-Dong, Bundang-Ku, Songnam-Si, Kyunggi-Do 463-746, Republic of Korea.

出版信息

Food Chem. 2016 Sep 1;206:85-91. doi: 10.1016/j.foodchem.2016.03.052. Epub 2016 Mar 16.

Abstract

We analyzed the physical properties and digestibility of apigenin-loaded emulsions as they passed through a simulated digestion model. As the emulsion passed through the simulated stages of digestion, the particle size and zeta potential of all the samples changed, except for the soybean oil-Tween 80 emulsion, in which zeta potential remained constant, through all stages, indicating that soybean oil-Tween 80 emulsions may have an effect on stability during all stages of digestion. Fluorescence microscopy was used to observe the morphology of the emulsions at each step. The in vivo pharmacokinetics revealed that apigenin-loaded soybean oil-Tween 80 emulsions had a higher oral bioavailability than did the orally administrated apigenin suspensions. These results suggest that W/O/W multiple emulsions formulated with soybean oil and tween 80 have great potential as targeted delivery systems for apigenin, and may enhance in vitro and in vivo bioavailability when they pass through the digestive tract.

摘要

我们分析了柚皮素负载乳液通过模拟消化模型时的物理性质和消化率。随着乳液通过模拟消化阶段,所有样品的粒径和zeta 电位都发生了变化,但大豆油-Tween 80 乳液除外,其 zeta 电位在所有阶段都保持不变,这表明大豆油-Tween 80 乳液可能在消化的所有阶段对稳定性有影响。荧光显微镜用于观察乳液在每个步骤的形态。体内药代动力学研究表明,负载柚皮素的大豆油-Tween 80 乳液的口服生物利用度高于口服柚皮素混悬液。这些结果表明,用大豆油和 Tween 80 配制的 W/O/W 多重乳液具有作为柚皮素靶向递送系统的巨大潜力,并且在通过消化道时可能会提高体外和体内的生物利用度。

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