ArticleCrystal growth & design2023
Tuning the Pharmacokinetic Performance of Quercetin by Cocrystallization.
Article in Crystal growth & design, 2023. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 9 papers.
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Who cites it
9 citing papers in PubMed.
- 40 years later: completion of the structural characterization of the anxiolytic drug buspirone HCl and solid-form landscape expansion.RSC advances · 2026Article
- A 'three-axis synergy' immunotherapeutic strategy for malignant bone tumors based on natural bioactives and bioactive materials.Bioactive materials · 2026Review
- Precipitation Inhibition by Small-Molecule Analogues To Sustain Drug Supersaturation.Molecular pharmaceutics · 2026Article
- Plant-Derived Compounds as Potential Sensitizers to Immunotherapy in Melanoma.International journal of molecular sciences · 2026Review
- Phase Diagram-Enabled Curcumin Isolation and Purification by Utilizing Resorcinol as Cocrystal Former and Additive.ACS omega · 2026Article
- Exploring the Multifunctional Roles of Betaine: Traditional Applications, Emerging Technologies, and Green Chemistry Innovations.Foods (Basel, Switzerland) · 2026Review
- Flavonoid-Based Cocrystals: A Comprehensive Study on Their Synthesis, Characterization, Physicochemical Properties and Applications.Molecules (Basel, Switzerland) · 2025Review
- A Combined Experimental and Modeling Workflow to Tune Surface Properties of Organic Materials via Cocrystallization.Chemistry of materials : a publication of the American Chemical Society · 2025Article
- Often neglected steps in transforming drug solubility from single measurement in pure water to physiologically-appropriate solubility-pH.ADMET & DMPK · 2025Article
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Authors and funding
10 authors.
Funding
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Abstract
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.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.