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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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“However, the clinical use of quercetin is limited due to its extremely low aqueous solubility, instability under physiological conditions and extensive metabolism by intestinal microflora, which resulted in low oral bioavailability, high inter-subjects variations and poor dose-response relationships [19,20,21,22].”
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“even loaded in normal MSN or other nanoparticles [34,35], so traditional nano-delivery of Qu may not significantly increase the therapeutic”
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“The flavonoids are plant phenolic compounds that exhibit strong antioxidant properties and are widely distributed throughout the plant kingdom; thus, flavonoids are a therapeutic option [25,26].”
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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.”
BackgroundFocus on the high therapeutic potentials of quercetin and its derivatives
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Co‐Encapsulation of EGCG and Quercetin in Liposomes for Optimum Antioxidant Activity
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“physiological effectiveness in the body (18).”
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“Qu is quickly conjugated with glucuronic acid and/or sulfate during first-pass metabolism (intestine-liver), and a portion of the metabolites is also methylated; the first investigation on the pharmacokinetics of Qu in humans suggested very poor oral bioavailability after a single oral dose (∼2%) [35].”
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“Curcumin, a natural phenolic product derived from the turmeric rhizome, has been indicated to have a variety of biological functions including anti-inflammation, anti-cancer, and antioxidation (Aggarwal et al., 2007; Anand et al., 2007).”
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“The therapeutic effects of QC and similar flavonoid compounds have been limited by drawbacks such as low bioavailability [13], instability [14], poor solubility [15], and inefficient biodistribution [16].”
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“However, poor solubility, low bioavailability, poor permeability and instability of quercetin considered as the biggest drawback since these properties limits it’s use as an anti-cancer agent (Smith et al. 2011; Cai et al. 2013).”
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Influence of naringenin on the biofilm formation of Streptococcus mutans
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“Quercetin appeared to have less cytotoxicity than ZnO/QR because of its poor in vitro bioavailability without a carrier to deliver on the target cells [45].”
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pH-sensitive polymeric nanoparticles of quercetin as a potential colon cancer-targeted nanomedicine
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“[34,35] 36 – 39] According to some research, quercetin, a dietary flavonoid which is the most studied flavonoid phytoconstituent, is absorbed in large levels in body.”
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“Quercetin Quercetin, a flavonoid isolated from various citrus fruits, tea, onions, and apples, exerts significant antioxidant, antiinflammatory, and antihypertensive activities.(36,145,146) Quercetin-loaded phosphatidylcholine liposomes (PCLs) found protective against myocardial injuries induced by peroxynitrite by di…”
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“Though many healthy systemic effects in humans have been attributed to QUE, it is barely absorbable in the gastrointestinal tract and as a result, in consequence, it accumulates in the lumen [13].”
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“QE has been reported as possessing a broad array of biological effects, including antioxidative, anti-inflammatory, antiapoptotic, hepatoprotective, renoprotective, neuroprotective, and cardioprotective effects (Cai et al., 2013; Liu et al., 2010, 2012; Morales et al., 2006; Prabu et al., 2013).”
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“Numerous approaches have been undertaken, involving the use of promising drug delivery systems such as inclusion complexes, liposomes, nanoparticles or micelles [63].”
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“Quercetin has been shown to have diverse pharmacological effects, which include antiinflammatory, anti-cancer, and anti-viral effects (Cai et al. 2013; Kim et al. 2015).”
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“In general, proanthocyanidins (Walle 2004; Cai et al. 2013; Williamson et al. 2018) and anthocyanins are the most poorly absorbed flavonoids whereas, Isoflavones are highly bioavailable among all other subclasses of flavonoids (Manach et al.”
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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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“Unfortunately, despite its promising therapeutic potential, 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).”
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“Firstly, bioavailability of quercetin is generally poor and it is affected by numerous factors [78, 153, 154].”
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“However, QT has the disadvantages of poor water and fat solubility and low bioavailability [12].”
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“curcumin nanoparticles, use of curcumin phospholipid complexes, and use of structural analogs of curcumin [6] .”
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“Despite Quer’s advantages, poor biopharmaceutical characteristic, namely: poor solubility and low bioavailability and instability, limited drastically therapeutic efficiency of quercetin [31].”
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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…”
BackgroundGreener therapeutic pH-sensing wound dressing based on Curcuma Longa and cellulose hydrogel
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Synthetic Biology towards Improved Flavonoid Pharmacokinetics
Sajid, M., Channakesavula, C. N., Stone, S. R., & Kaur, P. (2021) · Biomolecules · doi:10.3390/biom11050754 · Cited by 69
“Flavonoids generally possess low bioavailability when orally administered which significantly decreases their chance of attaining effective concentration in vivo [22].”
BackgroundPotential Targets for Colorectal Cancer Prevention
Temraz, S. N., Mukherji, D., & Shamseddine, A. I. (2013) · International Journal of Molecular Sciences · doi:10.3390/ijms140917279 · Cited by 66
“Hence, to improve its bioavailability, multiple approaches have been undertaken than involve improved drug delivery systems such as inclusion complexes, liposomes, nanoparticles or micelles, which appear to provide higher solubility and bioavailability [139].”
BackgroundChemical diversity of dietary phytochemicals and their mode of chemoprevention
Patra, S., Nayak, R., Patro, S., Pradhan, B., Sahu, B., Behera, C., Bhutia, S. K., & Jena, M. (2021) · Biotechnology Reports · doi:10.1016/j.btre.2021.e00633 · Cited by 66
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Impact of nanotechnology on the oral delivery of phyto-bioactive compounds
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Potential in vivo delivery routes of postbiotics
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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).”
BackgroundApplications of Alginate-Based Nanomaterials in Enhancing the Therapeutic Effects of Bee Products
Al-Hatamleh, M. A. I., Alshaer, W., Hatmal, M. M., Lambuk, L., Ahmed, N., Mustafa, M. Z., Low, S. C., Jaafar, J., Ferji, K., Six, J., et al. (2022) · Frontiers in Molecular Biosciences · doi:10.3389/fmolb.2022.865833 · Cited by 62
“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
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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