School of Traditional Chinese Material Medica, Shenyang Pharmaceutical University, Shenyang, China.
Faculty of Functional Food and Wine, Shenyang Pharmaceutical University, Shenyang, China.
Pharm Dev Technol. 2022 Sep;27(7):842-852. doi: 10.1080/10837450.2022.2123510. Epub 2022 Sep 16.
To improve the solubility and anti-hyperuricemia activity of the insoluble natural flavonoid isorhamnetin (ISO), an isorhamnetin phospholipid complex (ISO-PC) was prepared. ISO-PC was prepared through solvent evaporation and its prescription process was optimized. The formation of ISO-PC was verified via multiple characterization methods. Parameters such as drug loading, solubility, octanol-water partition coefficient, stability, and anti-hyperuricemia activity of ISO-PC were investigated. The complexation efficiency of ISO-PC was 95.1% ± 0.56%. The characterization results confirmed that ISO-PC was bound by intermolecular interactions between ISO and phospholipids. Compared with ISO, the solubility of ISO-PC in water and 1-octanol increased by 122 and 16.5 times, respectively. In addition, the octanol-water partition coefficient decreased to 1.08. Pharmacodynamic studies have reported that ISO-PC has a more significant effect on reducing serum uric acid levels and renal protection. In conclusion, the findings of this study suggested that ISO-PC could be used as a promising formulation to improve the solubility and the anti-hyperuricemia activity of ISO.
为提高不溶性天然类黄酮山柰素（ISO）的溶解度和抗高尿酸血症活性，制备了山柰素磷脂复合物（ISO-PC）。通过溶剂蒸发法制备 ISO-PC，并对其处方工艺进行优化。采用多种表征方法验证了 ISO-PC 的形成。考察了 ISO-PC 的载药量、溶解度、油水分配系数、稳定性和抗高尿酸血症活性等参数。ISO-PC 的包合效率为 95.1%±0.56%。表征结果证实 ISO-PC 是通过 ISO 和磷脂分子间的相互作用结合而成。与 ISO 相比，ISO-PC 在水中和 1-辛醇中的溶解度分别提高了 122 倍和 16.5 倍。此外，油水分配系数降低至 1.08。药效学研究报道，ISO-PC 对降低血尿酸水平和肾脏保护作用更显著。综上所述，本研究结果表明，ISO-PC 可作为提高 ISO 溶解度和抗高尿酸血症活性的一种有前途的制剂。
