Apigenin-oxymatrine binary co-amorphous mixture: Enhanced solubility, bioavailability, and anti-inflammatory effect

Area of Science:

• Food Science and Technology
• Pharmacology
• Materials Science

Background:

• Apigenin (APG) is a beneficial functional food ingredient with poor water solubility, limiting its bioavailability.
• Developing effective delivery systems is crucial for enhancing the efficacy of hydrophobic compounds like APG.

Purpose of the Study:

• To create a food-friendly co-amorphous mixture (CM) of apigenin (APG) and oxymatrine (OMT) to improve APG's solubility and oral bioavailability.
• To evaluate the physicochemical properties, solubility, dissolution, and anti-inflammatory effects of the APG-OMT CM.

Main Methods:

• Preparation and characterization of the APG-OMT co-amorphous mixture using powder X-ray diffraction and thermal analysis.
• Confirmation of hydrogen bonding interactions via vibrational spectroscopy and molecular dynamics simulations.
• Assessment of solubility, dissolution rates, and pharmacokinetic profiles, alongside in vivo anti-inflammatory activity evaluation.

Main Results:

• The APG-OMT CM formation was confirmed, with evidence of hydrogen bonding between APG and OMT.
• Significant improvements in APG solubility and dissolution rates were observed in the CM.
• The APG-OMT CM demonstrated enhanced oral bioavailability and a stronger anti-inflammatory effect compared to pure APG.

Conclusions:

• The co-amorphous formulation of apigenin and oxymatrine offers a promising strategy to overcome the bioavailability limitations of hydrophobic functional food ingredients.
• APG-OMT CM holds potential for application in functional foods, improving health benefits through enhanced delivery.
• This study presents a viable delivery system for hydrophobic compounds in the food industry.