ePrints

Tuning the Pharmacokinetic Performance of Quercetin by Cocrystallization

Lookup NU author(s): Dr Oisín KavanaghORCiD

Downloads

• Published version [.pdf]

Licence

This work is licensed under a Creative Commons Attribution 4.0 International License (CC BY 4.0).

Abstract

© 2023 The Authors. Published by American Chemical Society.Quercetin (QUE) is a widely studied nutraceutical with a number of potential therapeutic properties. Although QUE is abundant in the plant kingdom, its poor solubility (≤20 μg/mL) and poor oral bioavailability have impeded its potential utility and clinical development. In this context, cocrystallization has emerged as a useful method for improving the physicochemical properties of biologically active molecules. We herein report a novel cocrystal of the nutraceutical quercetin (QUE) with the coformer pentoxifylline (PTF) and a solvate of a previously reported structure between QUE and betaine (BET). We also report the outcomes of in vitro and in vivo studies of QUE release and absorption from a panel of QUE cocrystals: betaine (BET), theophylline (THP), l-proline (PRO), and novel QUEPTF. All cocrystals were found to exhibit an improvement in the dissolution rate of QUE. Further, the QUE plasma levels in Sprague-Dawley rats showed a 64-, 27-, 10- and 7-fold increase in oral bioavailability for QUEBET·MeOH, QUEPTF, QUEPRO, and QUETHP, respectively, compared to QUE anhydrate. We rationalize our in vivo and in vitro findings as the result of dissolution-supersaturation-precipitation behavior.

Publication metadata

Author(s): Haskins MM, Kavanagh ON, Sanii R, Khorasani S, Chen J-M, Zhang Z-Y, Dai X-L, Ren B-Y, Lu T-B, Zaworotko MJ

Publication type: Article

Publication status: Published

Journal: Crystal Growth and Design

Year: 2023

Volume: 23

Issue: 8

Pages: 6059–6066

Online publication date: 29/06/2023

Acceptance date: 02/04/2021

Date deposited: 02/08/2023

ISSN (print): 1528-7483

ISSN (electronic): 1528-7505

Publisher: American Chemical Society

URL: https://doi.org/10.1021/acs.cgd.3c00590

DOI: 10.1021/acs.cgd.3c00590

Altmetrics

Funding

Share