Novel cellulose-based amorphous solid dispersions enhance quercetin solution concentrations in vitro.

Area of Science:

• Pharmacology
• Materials Science
• Drug Delivery

Background:

• Quercetin (Q) is a health-benefiting flavonol with low bioavailability due to poor solubility and metabolism.
• Enhancing Q solution concentration in the small intestine can improve its bioavailability and efficacy.

Purpose of the Study:

• To develop amorphous solid dispersions (ASDs) of Q using cellulose derivatives to enhance its bioavailability.
• To evaluate the stability, pH-triggered release, and dissolution enhancement of Q-loaded ASDs.

Main Methods:

• Quercetin (Q) was incorporated into amorphous solid dispersions (ASDs) with cellulose esters (CCAB, HPMCAS, CASub) and polyvinylpyrrolidone (PVP).
• ASDs were characterized for stability against crystallization and pH-triggered release properties.
• Dissolution profiles and solution concentrations were assessed under intestinal pH conditions.

Main Results:

• Cellulose derivative-based ASDs provided stability against crystallization and exhibited pH-triggered release.
• Blends of CASub and CCAB with PVP further improved dissolution rates.
• The ASD formulation containing 10% Q:20% PVP:70% CASub demonstrated the most significant enhancement, increasing the area under the concentration/time curve (AUC) 18-fold compared to Q alone.

Conclusions:

• Novel ASDs incorporating Q with cellulose derivatives and PVP effectively enhance Q solution concentration under intestinal conditions.
• This ASD approach offers a promising strategy for significantly improving quercetin bioavailability and potential therapeutic efficacy in vivo.