Enhancing the potential preclinical and clinical benefits of quercetin through novel drug delivery systems

Khursheed, Rubiya; Singh, Sachin Kumar; Wadhwa, Sheetu; Gulati, Monica; Awasthi, Ankit

doi:10.1016/j.drudis.2019.11.001

Cited by 77 publications

(42 citation statements)

References 144 publications

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“…Quercetin is present in large quantities in many fruits and vegetables. According to several preclinical and clinical studies, this compound has exhibited some biological activities, namely: anti-inflammatory, antidiabetic, hepatoprotective, neuroprotective, antiplatelet, antibacterial potential, and acts to eliminate free radicals (Khursheed, Singh, Wadhwa, Gulati, & Awasthia 2019).…”

Section: Phenolic Profile Evaluated In Hydroethanolic Extract Of Quinmentioning

confidence: 99%

Chenopodium quinoa Willd. (quinoa) grains: A good source of phenolic compounds

Pereira

Cadavez

Barros

et al. 2020

Food Research International

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The ingestion of bioactive compounds has revealed health benefits, namely in the prevention and/or treatment of several diseases. This work aims to characterize the phenolic profile of three colour varieties of Chenopodium quinoa Willd. grains (black, red and white), and also evaluate their cytotoxic and antimicrobial activity. All varieties revealed the presence of phenolic compounds, namely, quercetin and kaempferol derivatives. In this study, quinoa grains did not reveal any anti-proliferative capacity in tumour cell lines, and, as expected, they were devoid of any toxicity. All of the analysed extracts possessed antibacterial and antifungal activities (inhibitory and bactericidal/fungicidal) against the microbial strains considered, exhibiting promising values of minimum bactericidal concentrations (mean MBC 0.153-0.916 mg/mL) and minimum fungicidal concentrations (mean MFC 0.211-0.884 mg/mL). Quinoa varieties represent a good source of bioactive compounds, interfering beneficially in the organism, specifically as antimicrobial agents. Thus, these extracts could be used in the development of bioactive ingredients.

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Section: Phenolic Profile Evaluated In Hydroethanolic Extract Of Quinmentioning

confidence: 99%

Chenopodium quinoa Willd. (quinoa) grains: A good source of phenolic compounds

Pereira

Cadavez

Barros

et al. 2020

Food Research International

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“…In this sense, numerous studies in vitro and in vivo pre-clinical studies have showed positive results. Regarding its action mechanisms, quercetin has been demonstrated to induce cell cycle arrest by regulating cyclin D1 and p53-related pathways; apoptosis trough the induction of pro-apoptotic factors and the decrease of anti-apoptotic ones; induces autophagy and inhibits proliferation, angiogenesis and metastasis [130,131]. These effects have been observed in different in vitro cell lines, including breast, ovarian, lung and colon cancer cells, among many others [130,132,133], and also in different in vivo mice models [134][135][136].…”

Section: Quercetinmentioning

confidence: 99%

“…However, in some cases, the results are limited due to the low solubility and bioavailability of this compound. To overcome these drawbacks, several delivery systems have been proposed for instance, lipids, nanoparticles, nanoemulsions, liposomes or micelles [131].…”

Section: Quercetinmentioning

confidence: 99%

Status and Challenges of Plant-Anticancer Compounds in Cancer Treatment

et al. 2021

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Nowadays, cancer is one of the deadliest diseases in the world, which has been estimated to cause 9.9 million deaths in 2020. Conventional treatments for cancer commonly involve mono-chemotherapy or a combination of radiotherapy and mono-chemotherapy. However, the negative side effects of these approaches have been extensively reported and have prompted the search of new therapeutic drugs. In this context, scientific community started to look for innovative sources of anticancer compounds in natural sources, including traditional plants. Currently, numerous studies have evaluated the anticancer properties of natural compounds derived from plants, both in vitro and in vivo. In pre-clinical stages, some promising compounds could be mentioned, such as the sulforaphane or different phenolic compounds. On the other hand, some phytochemicals obtained positive results in clinical stages and were further approved for cancer treatment, such as vinca alkaloids or the paclitaxel. Nevertheless, these compounds are not exempt of limitations, such as low solubility, restricted effect on their own, negative side-effects, etc. This review aims to compile the information about the current phytochemicals used for cancer treatment and also promising candidates, main action mechanisms and also reported limitations. In this sense, some strategies to face the limitations have been considered, such as nano-based formulations to improve solubility or chemical modification to reduce toxicity. In conclusion, although more research is still necessary to develop more efficient and safe phytochemical drugs, more of these compounds might be used in future cancer therapies.

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“…Quercetin is a naturally occurring antioxidant that has poor water solubility and as a result displays low permeation through the skin. [ 156 ] As a strategy to improve the intradermal delivery of this compound, Paleco et al. developed lipid MPs, using phosphatidylcholine and tristearin, that contained quercetin at a concentration of 11.7% w/w.…”

Section: Intradermal Administration Of Hydrophobic Drugsmentioning

confidence: 99%

Microarray Patches: Poking a Hole in the Challenges Faced When Delivering Poorly Soluble Drugs

Paredes

McKenna

Ramöller

et al. 2020

Adv Funct Materials

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Poorly soluble drugs constitute more than 60% of currently marketed pharmaceuticals with over two‐thirds of promising new chemical entities failing to enter a clinical setting due to solubility issues. Although oral formulations have made some impact, alternative enhancement strategies for administration of such molecules are actively sought. Over the last decade, innovation on a global scale has enabled the expansion of the frontiers of microarray patches (MAPs) further than ever before. Initially designed to load low doses of hydrophilic and potent therapeutic agents, MAPs are now becoming a viable strategy for the immediate and long‐acting delivery of poorly soluble drugs through the skin. This together with the advantages of transdermal administration over the oral and parenteral routes, make of MAPs an appealing platform for the development of products with increased patient compliance. Undoubtedly, MAPs will soon become a readily available therapeutic alternative, and experts from academia, industry and regulatory bodies are working together aiming to facilitate the progression of MAPs toward safe and effective clinical use. This review aims to highlight the ability of MAPs to deliver poorly soluble actives, discuss the mechanisms behind in‐skin drug absorption, and evaluate the future direction of the field.

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Enhancing the potential preclinical and clinical benefits of quercetin through novel drug delivery systems

Cited by 77 publications

References 144 publications

Chenopodium quinoa Willd. (quinoa) grains: A good source of phenolic compounds

Chenopodium quinoa Willd. (quinoa) grains: A good source of phenolic compounds

Status and Challenges of Plant-Anticancer Compounds in Cancer Treatment

Microarray Patches: Poking a Hole in the Challenges Faced When Delivering Poorly Soluble Drugs

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