Related Experiment Video
Updated: Jul 19, 2025
09:52
Optimizing the Growth of Endothiapepsin Crystals for Serial Crystallography Experiments
Published on: February 4, 2021
2.3K
Tuning the Pharmacokinetic Performance of Quercetin by Cocrystallization
Molly M Haskins1, Oisín N Kavanagh2, Rana Sanii1
1Department of Chemical Sciences, Bernal Institute, University of Limerick, Limerick V94 T9PX, Ireland.
Crystal Growth & Design
|August 7, 2023
Summary
Cocrystallization significantly enhances quercetin
Area of Science:
- Nutraceutical science
- Materials science
- Pharmacology
Background:
- Quercetin (QUE) is a nutraceutical with therapeutic potential.
- Poor solubility and bioavailability limit QUE's clinical use.
- Cocrystallization offers a strategy to improve physicochemical properties.
Purpose of the Study:
- To develop novel quercetin cocrystals.
- To evaluate the in vitro and in vivo performance of quercetin cocrystals.
- To enhance quercetin's dissolution and oral bioavailability.
Main Methods:
- Cocrystal formation using QUE with coformers like pentoxifylline (PTF) and betaine (BET).
- In vitro dissolution studies of QUE cocrystals.
- In vivo pharmacokinetic studies in Sprague-Dawley rats.
Main Results:
- All tested QUE cocrystals showed improved dissolution rates.
- Significant increases in oral bioavailability were observed: 64-fold (QUEBET·MeOH), 27-fold (QUEPTF), 10-fold (QUEPRO), and 7-fold (QUETHP).
- Findings attributed to dissolution-supersaturation-precipitation behavior.
Conclusions:
- Cocrystallization is an effective strategy to overcome QUE's poor solubility and bioavailability.
- Novel QUE cocrystals demonstrate enhanced therapeutic potential.
- Further development of cocrystal formulations for QUE is warranted.
