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