Preparation of an isorhamnetin phospholipid complex for improving solubility and anti-hyperuricemia activity

溶解度 异鼠李素 化学 分配系数 高尿酸血症 色谱法 溶剂 生物利用度 亲脂性 尿酸 类黄酮 药理学 山奈酚 有机化学 生物化学 抗氧化剂 医学
作者
Fengmao Zou,Honghui Zhao,Aijinxiu Ma,Danni Song,Xiangrong Zhang,Xu Zhao
出处
期刊:Pharmaceutical Development and Technology [Taylor & Francis]
卷期号:27 (7): 842-852 被引量:5
标识
DOI:10.1080/10837450.2022.2123510
摘要

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 in vivo 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.
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