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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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“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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“Quercetin (Figure 1) is a flavonoid that has been reported to be beneficial to human health, such as antioxidant, antiinflammatory, antitumor, antiviral and enzyme inhibitory actions (Cai et al., 2013; Chitkara et al., 2012; Landi-Librandi et al., 2012).”
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“On the other hand, quercetin has low bioavailability due to poor absorption [8,9] and rapid metabolism.”
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“Though it has antioxidant properties in vitro and is abundant in common foods, Q is poorly bioavailable and rapidly metabolized in vivo [41] so that the antioxidant activity cannot be the only mechanism behind Q’s cardiovascular protective effects.”
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“In addition, the polyphenolic ITPKA inhibitors are only weakly membrane permeable (own unpublished data and [16]).”
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Quercetin nanoformulations: recent advancements and therapeutic applications
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“Self-emulsifying drug delivery system (SEDDS) formulation are isotropic mixture of an oil, surfactant, co-surfactant and drug, that has the ability to form emulsion with water under gentle agitation as in the gastrointestinal tract.”
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Amin, A., Akhtar, M. S., Khalil, A. A. K., Ali, S., & Zaman, W. (2025) · Medicinal Chemistry Research · doi:10.1007/s00044-025-03508-z · Cited by 17
“For instance, quercetin — a well-studied fl avonoid, exhibits poor oral bioavailability in humans, typically ranging from 0.02% – 2%, owing to its low water solubility (approximately 0.01 mg/mL) and extensive fi rst-pass metabolism [121].”
InfluentialShereen Farhana, P., Francis, A. P., Gayathri, R., et al. (2024) · Journal of Advanced Oral Research · doi:10.1177/23202068241239150 · Cited by 11
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BackgroundOphthalmic Tethered Gold Yarnball‐Mediated Retained Drug Delivery for Eye Fundus Disease Treatment
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Effects of the Antioxidant Quercetin in an Experimental Model of Ulcerative Colitis in Mice
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“…effects of quercetin against degenerative diseases as demonstrated in a vast of cell-based in vitro, animal in vivo and human clinical settings (Cai et al., 2013; Gupta et al., 2016; Massi et al., 2017; Rani et al., 2015; Wang et al., 2018) (See Table 1 for Journal of Food Bioactives |…”
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“Because of quercetin ’ s short biological half-life, biochemical unpredictability, difficult to dissolve in water, and low the absorption of nutrients it might not be as useful in the dietary supplement and medicine sectors [85].”
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“This is due to some inherited properties, such as high hydrophobicity, low bioavailability and poor stability in physiological solutions [10,11].”
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Metadata
- 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 (medical) › Flavonoids in Medical Research
- Health Sciences › Medicine › Biochemistry (medical) › 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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