Development of liquiritigenin-phospholipid complex with the enhanced oral bioavailability

Area of Science:

• Pharmaceutical Sciences
• Drug Delivery Systems
• Natural Product Chemistry

Background:

• Liquiritigenin exhibits therapeutic potential but suffers from poor oral bioavailability.
• Developing effective delivery systems is crucial for maximizing liquiritigenin's therapeutic benefits.

Purpose of the Study:

• To develop and evaluate a liquiritigenin-phospholipid complex (LPC) to improve the oral bioavailability of liquiritigenin.
• To optimize the formulation and preparation process for LPC.

Main Methods:

• Single-factor test methodology for formulation optimization.
• Characterization using UV-Vis spectroscopy, DSC, FTIR, and PXRD.
• Pharmacokinetic studies in rats after oral administration.

Main Results:

• Optimized LPC preparation involved specific drug concentration, reaction time, temperature, drug-to-phospholipid ratio, and solvent (anhydrous ethanol).
• The optimized LPC demonstrated significantly enhanced lipid solubility compared to liquiritigenin alone.
• Oral administration of LPC in rats resulted in a 239% increase in AUC0-t compared to liquiritigenin.

Conclusions:

• The developed liquiritigenin-phospholipid complex (LPC) effectively enhances the oral bioavailability and lipid solubility of liquiritigenin.
• LPC represents a promising formulation for the clinical application and further development of liquiritigenin.