Quercetin-Eudragit® polymer complexes with enhanced loading, solubility, stability, and site-specific targeting.

Area of Science:

• Pharmacology
• Materials Science
• Drug Delivery

Background:

• Quercetin, a natural compound, shows promise for chronic disease prevention.
• Poor oral bioavailability of quercetin due to low solubility and permeability limits its therapeutic application.
• Targeted delivery systems are needed to enhance quercetin's effectiveness.

Purpose of the Study:

• To develop a polymer-based platform for targeted colon delivery of quercetin.
• To improve quercetin's solubility, stability, and oral absorption.
• To evaluate the efficacy of the developed quercetin-polymer complexes in colon cancer cells.

Main Methods:

• Quercetin complexes were prepared using co-precipitation with Eudragit® S100/L100/L100-55 polymers.
• Ethanol and polyvinyl alcohol were used as solvent and surfactant, respectively.
• Characterization included loading capacity, solubility, stability, and in vitro cytotoxicity assays.

Main Results:

• Polymer complexes exhibited high quercetin loading capacity (~315 μg/mL).
• Complexes showed amorphous nature, solubility at pH > 5.5, and significantly increased aqueous solubility (> 1 mg/mL).
• Enhanced stability (>30 h) and improved reduction in colon cancer cell viability (HCT116, HT29) were observed.

Conclusions:

• Successful development of a polymer-quercetin complex for targeted colon delivery.
• The developed complex demonstrates improved loading, solubility, stability, and enhanced anti-cancer activity.
• This platform offers a promising approach to overcome quercetin's bioavailability limitations.