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Lookup NU author(s): Dr Oisín KavanaghORCiD
This work is licensed under a Creative Commons Attribution 4.0 International License (CC BY 4.0).
© 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.
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
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