Cited by 423Drug Solubulity and Delivery SystemsFlavonoids in Medical ResearchPhytochemicals and Antioxidant Activities

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Bioavailability of Quercetin: Problems and Promises

Cai, X., Fang, Z., Dou, J., Yu, A., Zhai, G.·2013·Current Medicinal Chemistry

DOI 10.2174/09298673113209990120

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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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Background
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Background
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Background
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“Another compelling reason for inhaled QUE lies in the fact that oral administration of QUE is notoriously known for its resultant low bioavailability due to the significant first-pass metabolism of QUE in the gut and liver [22].”
Background
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Retracted
Development of self-microemulsifying drug delivery system for oral delivery of poorly water-soluble nutraceuticals
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Background
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“Autoreactive T cells that recognize self-antigens related to the myelin sheath pass through the blood-brain barrier (BBB) and secrete matrix metalloproteinases (MMPs), which can damage the extracellular matrix (ECM) [11].”
BackgroundInfluential
Quercetin nanocrystal-loaded alginate hydrogel patch for wound healing applications
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“QUE is barely absorbable in the gastrointestinal tract, and as a result, it accumulates in the colon lumen [11].”
Background
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“However, the therapeutic efﬁcacy of the SD is likely to be limited by rapid elimination of quercetin via faeces and urine (Cai et al., 2013).”
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“loba, was classified in Class IV, characterized by both low solubility and permeability, in agreement with the reported low bioavailability of Que [11].”
BackgroundResult
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“It also solves the problem of low bioavailability of intraperitoneal or intravenous infusions of quercetin [38].”
Background
Carriers Based on Zein-Dextran Sulfate Sodium Binary Complex for the Sustained Delivery of Quercetin
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“These potent properties, however, are limited due to inferior water-solubility and poor bioavailability of quercetin (Cai et al., 2013).”
Background
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“However, the development of Que-based chemotherapeutics has been essentially hindered by the inadequate bioavailability and weak water solubility of this compound, besides its extensive metabolic conversion in the human body (Ulusoy and Sanlier 2020; Cai et al. 2013).”
Background
Facile Synthesis and Characterization of Quercetin-Loaded Alginate Nanoparticles for Enhanced In Vitro Anticancer Effect Against Human Leukemic Cancer U937 Cells
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“However, these properties are limited by poor oral bioavailability and scarce distribution in the organism as a whole and to the brain [13].”
Background
Peroxisome proliferator-activated receptor gamma as a therapeutic target for hepatocellular carcinoma: Experimental and clinical scenarios
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Antitumor activity and safety evaluation of nanaparticle-based delivery of quercetin through intravenous administration in mice
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“However, due to its poor water solubility, chemical stability, and absorption properties, quercetin’s bioavailability is usually less than 10% [187].”
Background
Therapeutic Efficacy of Quercetin and Its Nanoformulation Both the Mono‐ or Combination Therapies in the Management of Cancer: An Update with Molecular Mechanisms
Eity, T. A., Bhuia, M. S., Chowdhury, R., Ahmmed, S., Sheikh, S., Akter, R., & Islam, M. T. (2024) · Journal of Tropical Medicine · doi:10.1155/2024/5594462 · Cited by 37
“…bioavailability of quercetin, various strategies have been employed, including the application of potential drug delivery methods such as inclusion complexes, liposomes, nanoparticles, or micelles, which have been demonstrated to increase efcacy, stability, solubility, and bioavailability [70, 73].”
BackgroundMethod
Effect of quercetin on lipid membrane rigidity: assessment by atomic force microscopy and molecular dynamics simulations
Eid, J., Jraij, A., Greige‐Gerges, H., et al. (2021) · BBA Advances · doi:10.1016/j.bbadva.2021.100018 · Cited by 33
Hepatotoxicity and renal toxicity induced by radiation and the protective effect of quercetin in male albino rats
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“Quercetin has been reported to have a wide range of biological effects, including anti-apoptotic, anti-inflammatory, anti-oxidative, renoprotective, hepatoprotective, cardioprotective, and neuroprotective effects (Morales et al. 2006; Liu et al. 2010; Cai et al. 2013; Prabu et al. 2013).”
Background
Recent insights into oxidative metabolism of quercetin: catabolic profiles, degradation pathways, catalyzing metalloenzymes and molecular mechanisms
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“…reviews discussed its clinical prospects (Dajas 2012; Russo et al. 2012; Ranawat, Pathak, and Khanduja 2013; D’Andrea 2015), bioavailability issue (Cai et al. 2013; Guo and Bruno 2015; Carullo, Badolato, and Aiello 2018; Khursheed et al. 2020), metabolism behavior (Terao, Murota, and Kawai 2011;…”
Background
Plant‐derived flavonoids are a potential source of drugs for the treatment of liver fibrosis
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“For example, quercetin's structure contains four phenolic hydroxyl groups, making it susceptible to glucuronidation and sulfation in the gut, which reduces its gastrointestinal permeability (Cai et al., 2013; Fang et al., 2017).”
Background
Quercetagetin-loaded zein-propylene glycol alginate composite particles induced by calcium ions: Structural comparison between colloidal dispersions and lyophilized powders after in vitro simulated gastraintestinal digestion
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“Additionally, the use of a thermosensitive hydrogel system could assist in overcoming the limitation of poor water solubility of quercetin, its destabilization in physiological media and hence its poor bioavailability [33,34].”
Background
Isoquercitrin Attenuates Steatohepatitis by Inhibition of the Activated NLRP3 Inflammasome through HSP90
Ma, J., Li, M., Yang, T., Deng, Y., Ding, Y., Guo, T., & Shang, J. (2023) · International Journal of Molecular Sciences · doi:10.3390/ijms24108795 · Cited by 31
“The results have shown the poor uptake and rapid metabolism of quercetin, which severely limits its further application [17].”
Background
Synthesis of novel biocompatible resorcinarene based nanosized dendrimer-vesicles for enhanced anti-bacterial potential of quercetin
Rehman, K., Ali, I., El‐Haj, B. M., et al. (2021) · Journal of Molecular Liquids · doi:10.1016/j.molliq.2021.116921 · Cited by 29
Potential applications of nanomedicine for treating Parkinson's disease
Shankar, J., Geetha, K. M., & Wilson, B. (2021) · Journal of Drug Delivery Science and Technology · doi:10.1016/j.jddst.2021.102793 · Cited by 29
Curcumin loaded Ag–TiO 2 -halloysite nanotubes platform for combined chemo-photodynamic therapy treatment of cancer cells
Nyankson, E., Awuzah, D., Tiburu, E. K., et al. (2022) · RSC Advances · doi:10.1039/d2ra05777h · Cited by 28
Quercetin Derivatives as Potential Therapeutic Agents: An Updated Perspective on the Treatment of Nicotine-Induced Non-Small Cell Lung Cancer
Alsharairi, N. A. (2023) · International Journal of Molecular Sciences · doi:10.3390/ijms242015208 · Cited by 28
“The chemical structures of these QDs are presented in Figure 2. approaches have been recommended to enhance Q bioavailability, including nanoparticles, micelles, inclusion complexes, and liposomes [24].”
Background
PEG4000 modified liposomes enhance the solubility of quercetin and improve the liposome functionality: in vitro characterization and the cellular efficacy
Demirbolat, G. M., Erdoğan, Ö., Coşkun, G. P., et al. (2022) · TURKISH JOURNAL OF CHEMISTRY · doi:10.55730/1300-0527.3411 · Cited by 27
Quercetin: Potential antidiabetic effects through enzyme inhibition and starch digestibility
Günal‐Köroğlu, D., Çatalkaya, G., Yusufoğlu, B., et al. (2024) · Food Safety and Health · doi:10.1002/fsh3.12066 · Cited by 27
Xiyangshen Sanqi Danshen granules attenuated D-gal-induced C57BL/6J mouse aging through the AMPK/SIRT1 signaling pathway
Yin, Z., Tian, L., Kou, W., Cao, G., Wang, L., Xia, Y.-F., Lin, Y., Tang, S., Zhang, J., & Yang, H. (2024) · Phytomedicine · doi:10.1016/j.phymed.2024.156213 · Cited by 28
Fabrication of Nanosuspensions to Improve the Oral Bioavailability of Total Flavones from Hippophae rhamnoides L. and their Comparison with an Inclusion Complex
Tian, R., Wang, H., Xiao, Y., et al. (2020) · AAPS PharmSciTech · doi:10.1208/s12249-020-01788-9 · Cited by 27
Pellets containing quercetin amino acid co-amorphous mixture for the treatment of pain: Formulation, optimization, in-vitro and in-vivo study
Hatwar, P., Pathan, I. B., Chishti, N. A. H., et al. (2021) · Journal of Drug Delivery Science and Technology · doi:10.1016/j.jddst.2021.102350 · Cited by 27
Epimedii Herba: An ancient Chinese herbal medicine in the prevention and treatment of rheumatoid arthritis
Zhang, L., Yan, Y., He, J., et al. (2022) · Frontiers in Chemistry · doi:10.3389/fchem.2022.1023779 · Cited by 27
“For example, bioavailability of quercetin is pharmaceutically characterized as poor solubility, low bioavailability, poor permeability and instability (Cai et al., 2013).”
Background
Revolutionizing neurotherapeutics: Nanocarriers unveiling the potential of phytochemicals in Alzheimer's disease
Kamath, A. P., Nayak, P. G., John, J., Mutalik, S., Balaraman, A. K., & Nandakumar, K. (2024) · Neuropharmacology · doi:10.1016/j.neuropharm.2024.110096 · Cited by 32
“At present, nanotechnology is being utilized to develop nanosized structures to facilitate numerous procedures within the field of medicine, including the delivery of drugs (Cai et al., 2013; Rajesh R and Dhanaraj, 2023; Riva et al., 2019)”
Method
Impact of quercetin-induced changes in drug-metabolizing enzyme and transporter expression on the pharmacokinetics of cyclosporine in rats
Liu, Y., Luo, X., Yang, C., et al. (2016) · Molecular Medicine Reports · doi:10.3892/mmr.2016.5616 · Cited by 26
“It exhibits antioxidant, anti‐inflammatory, anticancer, neuroprotective, anti-anaphylaxis and anti-aging effects (5-7).”
Preparation and characterization of quercetin-polyvinylpyrrolidone K-30 spray dried solid dispersion
Febriyenti, F., Indra, P., Zaini, E., Ismed, F., & Lucida, H. (2020) · Journal of Pharmacy & Pharmacognosy Research · doi:10.56499/jppres19.729_8.2.127 · Cited by 26
“(Moon et al., 2008; Cai et al., 2013).”
Background
Quercetin Derivatives in Combating Spinal Cord Injury: A Mechanistic and Systematic Review
Fakhri, S., Gravandi, M. M., Abdian, S., Moradi, S. Z., & Echeverría, J. (2022) · Life · doi:10.3390/life12121960 · Cited by 26
Principal Component Analysis (PCA) of Molecular Descriptors for Improving Permeation through the Blood–Brain Barrier of Quercetin Analogues
Pavlović, N., Sopta, N. M., Mitrović, D., Zaklan, D., Tomás, A., Stilinović, N., & Vukmirović, S. (2023) · International Journal of Molecular Sciences · doi:10.3390/ijms25010192 · Cited by 26
“Numerous chemical and formulation strategies to surmount these obstacles have emerged [14], including the identification of quercetin analogues that possess similar pharmacological activity but more favorable pharmacokinetic characteristics using in silico techniques [15,16].”
Background
Thermodynamics of complex formation between hydroxypropyl-β-cyclodextrin and quercetin in water–ethanol solvents at T = 298.15 K
Усачева, Т. Р., Нурмахмадович, К. Д., Beregova, D., Gamov, G. A., Sharnin, V. A., Biondi, M., Mayol, L., D’Aria, F., & Giancola, C. (2019) · Journal of Thermal Analysis and Calorimetry · doi:10.1007/s10973-019-08136-5 · Cited by 28
Quercetin-Amino Acid Conjugates are Promising Anti-Cancer Agents in Drug Discovery Projects
Dobrydnev, A. V., Tkachuk, T. M., Атаманюк, В. П., & Popova, M. V. (2019) · Mini-Reviews in Medicinal Chemistry · doi:10.2174/1389557519666191009152007 · Cited by 23
Effect of a Drug Delivery System Made of Quercetin Formulated into PEGylation Liposomes on Cervical Carcinoma In Vitro and In Vivo
Li, J., Li, Z., Gao, Y., et al. (2021) · Journal of Nanomaterials · doi:10.1155/2021/9389934 · Cited by 25
“However, its poor bioavailability, low aqueous solubility, and low stability limit its wide application in pharmaceutics [4].”
Background
Anti-amyloidogenic property of gold nanoparticle decorated quercetin polymer nanorods in pH and temperature induced aggregation of lysozyme
Rananaware, P., Pandit, P., Naik, S., Mishra, M., Keri, R. S., & Brahmkhatri, V. P. (2022) · RSC Advances · doi:10.1039/d2ra03121c · Cited by 26
Strategies for Regulating the Release Kinetics of Bioactive Compounds from Biopolymeric Hydrogels
Rahman, M. M., Teimouri, S., Roy, P. R., Raposo, A., Alturki, H. A., & Kasapis, S. (2025) · Gels · doi:10.3390/gels11120986 · Cited by 26
“Nevertheless, its use in the pharmaceutical industry is constrained by several factors, including inadequate solubility, low bioavailability, limited permeability, and instability within the gastrointestinal tract [64].”
CHNQ, a novel 2-Chloro-1,4-naphthoquinone derivative of quercetin, induces oxidative stress and autophagy both in vitro and in vivo
Enayat, S., Ceyhan, M. Ş., Taşkoparan, B., Štefek, M., & Banerjee, S. (2016) · Archives of Biochemistry and Biophysics · doi:10.1016/j.abb.2016.03.004 · Cited by 24
Self-emulsifying formulations to augment therapeutic efficacy of nutraceuticals: From concepts to clinic
Dhritlahre, R. K., Ruchika, Padwad, Y. S., & Saneja, A. (2021) · Trends in Food Science & Technology · doi:10.1016/j.tifs.2021.06.046 · Cited by 22
A highly versatile fungal glucosyltransferase for specific production of quercetin-7-O-β-d-glucoside and quercetin-3-O-β-d-glucoside in different hosts
Ren, J., Tang, W., Barton, C. D., et al. (2021) · Applied Microbiology and Biotechnology · doi:10.1007/s00253-021-11716-x · Cited by 24
“It exerts promising pharmacological properties, such as anticancer, anti-inflammatory, antiviral, and antihypertensive properties (Cai et al. 2013; Ma et al. 2013).”
Background
Potentiation of Cisplatin Cytotoxicity in Resistant Ovarian Cancer SKOV3/Cisplatin Cells by Quercetin Pre-Treatment
Hasan, A. A., Kalinina, E. V., Nuzhina, J., Volodina, Y. L., Shtil, A. A., & Tatarskiy, V. V. (2023) · International Journal of Molecular Sciences · doi:10.3390/ijms241310960 · Cited by 24
“However, the clinical application of QU is limited due to its poor solubility, low bioavailability, poor permeability, and instability [19].”
Background
An eco-friendly one-pot extraction process for curcumin and its bioenhancer, piperine, from edible plants in exosome-like nanovesicles
Kumar, M. N., Kalarikkal, S. P., Bethi, C. M. S., Singh, S. N., Janakiraman, N., & Sundaram, G. M. (2023) · Green Chemistry · doi:10.1039/d3gc01287e · Cited by 24
Smart PLGA nanoparticles loaded with Quercetin: Cellular uptake and in-vitro anticancer study
Halder, A., Mukherjee, P., Ghosh, S., et al. (2018) · Materials Today Proceedings · doi:10.1016/j.matpr.2017.10.156 · Cited by 24
Inhibition of the Proliferation and Invasion of C6 Glioma Cells by Tricin via the Upregulation of Focal-Adhesion-Kinase-Targeting MicroRNA-7
Chung, D.-J., Wang, C., Yeh, C., et al. (2018) · Journal of Agricultural and Food Chemistry · doi:10.1021/acs.jafc.8b00604 · Cited by 24
Thermodynamic and acoustic studies of quercetin with sodium dodecyl sulfate in hydro-ethanolic solvent systems: A flavonoid-surfactant interaction study
Abbot, V., & Sharma, P. (2020) · Chemical Physics · doi:10.1016/j.chemphys.2020.110921 · Cited by 23
Potential molecular and graphene oxide chelators to dissolve amyloid-β plaques in Alzheimer's disease: a density functional theory study
Liu, C., & Luo, X. (2021) · Journal of Materials Chemistry B · doi:10.1039/d0tb02985h · Cited by 23

Authors: Cai, X., Fang, Z., Dou, J., Yu, A., & Zhai, G.
Affiliations: Shandong University (CN)
Corresponding author: Fang, Z.
Zhai, G.
ORCID: Cai, X.
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)
DOI: 10.2174/09298673113209990120
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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Bioavailability of Quercetin: Problems and Promises

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