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

Abstract

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.

Graphical Abstract

Keywords:

• Isorhamnetin
• phospholipid complex
• hyperuricemia
• solubility
• characterization

Author contributions

FZ: Investigation, Data curation, Methodology, Writing-original draft, Writing-review & editing, Formal analysis. HZ: Methodology project, Formal analysis. AM: Methodology project, Formal analysis. DS: Methodology project. XZ: Project administration, Methodology, Writing – review & editing. XZ: Supervision, Project administration, Methodology, Writing – review & editing.

Disclosure statement

No potential conflict of interest was reported by the authors.

Additional information

Funding

Young and Middle Aged Teachers’ Career Development Support Project of Shenyang Pharmaceutical University [ZQN2019005]; Livelihood Plan Project of Department of Science and Technology of Liaoning Province [2021JH2/10300069]; Department of Education of Liaoning Province [LJKZ0918].