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槲皮素通过α-葡萄糖基甜菊纳米聚集体与亲水性聚合物相互作用提高其溶解度和渗透性。

Solubility and Permeability Improvement of Quercetin by an Interaction Between α-Glucosyl Stevia Nanoaggregates and Hydrophilic Polymer.

机构信息

Laboratory of Formulation Design and Pharmaceutical Technology, Osaka University of Pharmaceutical Sciences, 4-20-1 Nasahara, Takatsuki, Osaka 569-1094, Japan.

Laboratory of Natural Product Research, Osaka University of Pharmaceutical Sciences, 4-20-1 Nasahara, Takatsuki, Osaka 569-1094, Japan.

出版信息

J Pharm Sci. 2019 Jun;108(6):2033-2040. doi: 10.1016/j.xphs.2019.01.007. Epub 2019 Jan 14.

Abstract

The effect of composite formation between α-glucosyl stevia (Stevia-G) and hydrophilic polymers on solubility and permeability enhancement of quercetin hydrate (QUE) was evaluated. Polyvinylpyrrolidone K-30 (PVP), hydroxypropyl methylcellulose 2910-E (HPMC), and hydroxypropyl cellulose SSL (HPC) were selected as candidate hydrophilic polymers. Fluorescence studies with pyrene and curcumin suggested composite formation occurs between Stevia-G aggregate and polymers. Furthermore, the strength of interaction between Stevia-G aggregate and polymers was as follows: PVP > HPMC > HPC. Evaporated particles (EVPs) of QUE with Stevia-G and polymers showed synergic QUE solubility enhancement. Solubility of QUE from the EVPs was enhanced in the following order: Stevia-G/PVP > Stevia-G/HPMC > Stevia-G/HPC, in accordance with the degree of interaction. Enhanced membrane permeability of QUE from the EVPs of Stevia-G/PVP was confirmed using Caco-2 cells. The amount of QUE that permeated Caco-2 cells from the EVPs of Stevia-G/PVP was 13.7-, 4.7-, and 2.1-fold higher than that of the untreated QUE powder, EVPs of Stevia-G, and EVPs of PVP, respectively. These results indicated that the composite formed by Stevia-G and PVP can dramatically enhance the solubility and membrane permeability of QUE.

摘要

研究了α-葡萄糖基甜菊糖苷(Stevia-G)与亲水性聚合物形成复合物对槲皮素水合物(QUE)溶解度和渗透性的影响。选择聚乙烯吡咯烷酮 K-30(PVP)、羟丙基甲基纤维素 2910-E(HPMC)和羟丙基纤维素 SSL(HPC)作为候选亲水性聚合物。芘和姜黄素的荧光研究表明,Stevia-G 聚集体与聚合物之间发生了复合形成。此外,Stevia-G 聚集体与聚合物之间相互作用的强度如下:PVP>HPMC>HPC。具有 Stevia-G 和聚合物的 QUE 的蒸发颗粒(EVPs)显示出 QUE 溶解度的协同增强。从 EVPs 增强的 QUE 溶解度顺序如下:Stevia-G/PVP>Stevia-G/HPMC>Stevia-G/HPC,与相互作用程度一致。使用 Caco-2 细胞证实了从 Stevia-G/PVP 的 EVPs 中 QUE 增强的膜渗透性。从 Stevia-G/PVP 的 EVPs 中穿过 Caco-2 细胞的 QUE 量分别比未处理的 QUE 粉末、Stevia-G 的 EVPs 和 PVP 的 EVPs 高 13.7、4.7 和 2.1 倍。这些结果表明,Stevia-G 和 PVP 形成的复合物可以显著提高 QUE 的溶解度和膜渗透性。

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