Both quercetin and resveratrol are promising plant-derived compounds with various well-described biological activities; however, they are categorized as having low aqueous solubility and labile natural compounds. The purpose of the present study was to propose a drug delivery system to enhance the oral bioavailability of combined quercetin and resveratrol. The suitable self-microemulsifying formulation containing quercetin together with resveratrol comprised 100 mg Capryol 90, 700 mg Cremophor EL, 200 mg Labrasol, 20 mg quercetin, and 20 mg resveratrol, which gave a particle size of 16.91 ± 0.08 nm and was stable under both intermediate and accelerated storage conditions for 12 months. The percentages of release for quercetin and resveratrol in the self-microemulsifying formulation were 75.88 ± 1.44 and 86.32 ± 2.32%, respectively, at 30 min. In rats, an in vivo pharmacokinetics study revealed that the area under the curve of the self-microemulsifying formulation containing quercetin and resveratrol increased approximately ninefold for quercetin and threefold for resveratrol compared with the unformulated compounds. Moreover, the self-microemulsifying formulation containing quercetin and resveratrol slightly enhanced the in vitro antioxidant and cytotoxic effects on AGS, Caco-2, and HT-29 cells. These findings demonstrate that the self-microemulsifying formulation containing quercetin and resveratrol could successfully enhance the oral bioavailability of the combination of quercetin and resveratrol without interfering with their biological activities. These results provide valuable information for more in-depth research into the utilization of combined quercetin and resveratrol.

中文翻译：

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使用液体自微乳化给药系统提高槲皮素/白藜芦醇组合的口服生物利用度和生物活性

槲皮素和白藜芦醇都是具有多种生物活性的有前途的植物衍生化合物。然而，它们被归类为具有低水溶性和不稳定的天然化合物。本研究的目的是提出一种药物递送系统，以提高槲皮素和白藜芦醇组合的口服生物利用度。包含槲皮素和白藜芦醇的合适自微乳化制剂包含 100 mg Capryol 90、700 mg Cremophor EL、200 mg Labrasol、20 mg 槲皮素和 20 mg 白藜芦醇，其粒径均为 16.91 ± 0.08 nm 且在波长范围内稳定中间和加速储存条件为 12 个月。自微乳化制剂中槲皮素和白藜芦醇的释放百分比在 30 分钟时分别为 75.88 ± 1.44 和 86.32 ± 2.32%。在大鼠中，一项体内药代动力学研究表明，与未配制的化合物相比，含有槲皮素和白藜芦醇的自微乳化制剂的曲线下面积增加了大约 9 倍和 3 倍的白藜芦醇。此外，含有槲皮素和白藜芦醇的自微乳化制剂略微增强了对 AGS、Caco-2 和 HT-29 细胞的体外抗氧化和细胞毒作用。这些发现表明，含有槲皮素和白藜芦醇的自微乳化制剂可以成功地提高槲皮素和白藜芦醇组合的口服生物利用度，而不会干扰它们的生物活性。这些结果为更深入地研究槲皮素和白藜芦醇组合的利用提供了有价值的信息。一项体内药代动力学研究表明，与未配制的化合物相比，含有槲皮素和白藜芦醇的自微乳化制剂的曲线下面积增加了槲皮素的约九倍和白藜芦醇的三倍。此外，含有槲皮素和白藜芦醇的自微乳化制剂略微增强了对 AGS、Caco-2 和 HT-29 细胞的体外抗氧化和细胞毒作用。这些发现表明，含有槲皮素和白藜芦醇的自微乳化制剂可以成功地提高槲皮素和白藜芦醇组合的口服生物利用度，而不会干扰它们的生物活性。这些结果为更深入地研究槲皮素和白藜芦醇组合的利用提供了有价值的信息。一项体内药代动力学研究表明，与未配制的化合物相比，含有槲皮素和白藜芦醇的自微乳化制剂的曲线下面积增加了槲皮素的约九倍和白藜芦醇的三倍。此外，含有槲皮素和白藜芦醇的自微乳化制剂略微增强了对 AGS、Caco-2 和 HT-29 细胞的体外抗氧化和细胞毒作用。这些发现表明，含有槲皮素和白藜芦醇的自微乳化制剂可以成功地提高槲皮素和白藜芦醇组合的口服生物利用度，而不会干扰它们的生物活性。这些结果为更深入地研究槲皮素和白藜芦醇组合的利用提供了有价值的信息。