Bioavailability of Quercetin: Problems and Promises
Abstract
Quercetin (QC) is a typical plant flavonoid, possesses diverse pharmacologic effects including antiinflammatory, antioxidant, anti-cancer, anti-anaphylaxis effects and against aging. However, the application of QC in pharmaceutical field is limited due to its poor solubility, low bioavailability, poor permeability and instability. To improve the bioavailability of QC, numerous approaches have been undertaken, involving the use of promising drug delivery systems such as inclusion complexes, liposomes, nanoparticles or micelles, which appear to provide higher solubility and bioavailability. Enhanced bioavailability of QC in the near future is likely to bring this product to the forefront of therapeutic agents for treatment of human disease.
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Clinical use of quercetin is limited probably due to poor BBB permeability, low bioavailability, and rapid metabolism.
“a clinical approach with the use of quercetin has been quite limited probably due to its poor permeability of the BBB, low bioavailability, and rapid metabolism (Cai et al., 2013)”
From Exploring the Therapeutic Potential of Phytochemicals in Alzheimer’s Disease: Focus on Polyphenols and Monoterpenes (2022) · cites this paper as Cai et al., 2013
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“that can quench ROS, reactive nitrogen species, and other radicals.(21,22) Li et al showed that low concentration of Que decreased the cytotoxic effect of cisplatin by reducing intracellular ROS in ovarian cancer.”
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“However, some drawbacks limit the pharmaceutical use of QT, such as poor water solubility (≈10 μg/mL), scarce bioavailability, and chemical instability [11].”
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“However, QT has the disadvantages of poor water and fat solubility and low bioavailability [12].”
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BackgroundQuercetin as an Emerging Anti-Melanoma Agent: A Four-Focus Area Therapeutic Development Strategy
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“However, its anti-inflammatory and chondroprotective properties have been inconsistent attributed to its low bioavailability, solubility, and high rate of metabolism in the gastrointestinal tract.(19,39) The current study aimed to employ mPEG-PA hydrogel as a drug delivery system to localize and prolong the effect of…”
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“…most of the therapeutic biomolecules are more unstable chemical components in comparison with synthetic chemicals, it is vital to carry the therapeutic biomolecules to the treatment site until it is broken down throughout the pharmacokinetics’ pathways (Cai et al. 2013; Yoshioka and Ochiya 2019).”
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“Despite the high therapeutic potential of quercetin, it has poor solubility, bioavailability, bioaccessibility and stability, which has encouraged researchers to utilize several nano-based drug delivery systems to overcome these obstacles (Cai et al., 2013; Wang et al., 2021).”
Background
- Authors
- Cai, X., Fang, Z., Dou, J., Yu, A., & Zhai, G.
- Affiliations
- Shandong University (CN)
- Corresponding author
- Fang, Z.
- Zhai, G.
- Venue
- Current Medicinal Chemistry
- Publisher
- Bentham Science Publishers Ltd.
- Published
- 2013-05-01
- Volume
- 20
- Issue
- 20
- Pages
- 2572-2582
- ISSN
- 0929-8673 (ISSN-L)
- OpenAlex
- W2133019478
- Cited by
- 423
- References
- 0
- Citations by year
- 2026: 39 · 2025: 39 · 2024: 42 · 2023: 53 · 2022: 46 · 2021: 42 · 2020: 42 · 2019: 29 · 2018: 22 · 2017: 15 · 2016: 22 · 2015: 17 · 2014: 11 · 2013: 4
- FWCI
- 10.83
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Current Medicinal Chemistry (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Drug Solubulity and Delivery Systems
- Health Sciences › Medicine › Pharmacology › Flavonoids in Medical Research
- Health Sciences › Medicine › Biochemistry › Phytochemicals and Antioxidant Activities
- Keywords
- quercetin, bioavailability, flavonoids, drug delivery systems, inclusion complexes, liposomes, nanoparticles, micelles, solubility enhancement, permeability, antioxidant activity, anti-inflammatory activity, anticancer activity
- MeSH terms
- Biocompatible Materials, Biological Availability, Drug Carriers, Half-Life, Humans, Liposomes, Micelles, Prodrugs, Quercetin, Solubility, Nanoparticles
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