Fisetin—In Search of Better Bioavailability—From Macro to Nano Modifications: A Review

Szymczak, Joanna; Cielecka-Piontek, Judyta

doi:10.3390/ijms241814158

Cited by 17 publications

(4 citation statements)

References 127 publications

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“…Consequently, researchers have explored various strategies to enhance the solubility of FIS, aiming to optimise its delivery and efficacy. In this review, the authors collected the most popular techniques for improving the solubility of FIS [26]. One approach involves the utilisation of nanoparticles, which can encapsulate FIS and improve its solubility while also providing controlled release properties [27,28].…”

Section: Introductionmentioning

confidence: 99%

A Fisetin Delivery System for Neuroprotection: A Co-Amorphous Dispersion Prepared in Supercritical Carbon Dioxide

Sip,

Rosiak,

Sip

et al. 2023

Antioxidants

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Fisetin (FIS), a senolytic flavonoid, mitigates age-related neuroprotective changes. An amorphous FIS dispersion with a co-carrier was prepared using supercritical fluid extraction with carbon dioxide (scCO2). Characterisation, including powder X-ray diffraction and Fourier-transform infrared spectroscopy, confirmed amorphization and assessed intermolecular interactions. The amorphous FIS dispersion exhibited enhanced solubility, dissolution profiles, and bioavailability compared to the crystalline form. In vitro, the amorphous FIS dispersion demonstrated antioxidant activity (the ABTS, CUPRAC, DDPH, FRAP assays) and neuroprotective effects by inhibiting acetylcholinesterase and butyrylcholinesterase. FIS modulated gut microbiota, reducing potentially pathogenic gram-negative bacteria without affecting probiotic microflora. These improvements in solubility, antioxidant and neuroprotective activities, and gut microbiome modulation suggest the potential for optimising FIS delivery systems to leverage its health-promoting properties while addressing oral functionality limitations.

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Section: Introductionmentioning

confidence: 99%

A Fisetin Delivery System for Neuroprotection: A Co-Amorphous Dispersion Prepared in Supercritical Carbon Dioxide

Sip,

Rosiak,

Sip

et al. 2023

Antioxidants

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“…It has to be considered, though, that the bioavailability of fisetin after oral administration is poor, so it is necessary to develop an effective delivery method to enhance its therapeutic potential in treatment of a particular disease, e.g. , using nanotechnologies [ 88 ].…”

Section: Senotherapeuticsmentioning

confidence: 99%

Mini-encyclopedia of mitochondria-relevant nutraceuticals protecting health in primary and secondary care—clinically relevant 3PM innovation

Golubnitschaja,

Kapinova,

Sargheini

et al. 2024

EPMA Journal

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Despite their subordination in humans, to a great extent, mitochondria maintain their independent status but tightly cooperate with the “host” on protecting the joint life quality and minimizing health risks. Under oxidative stress conditions, healthy mitochondria promptly increase mitophagy level to remove damaged “fellows” rejuvenating the mitochondrial population and sending fragments of mtDNA as SOS signals to all systems in the human body. As long as metabolic pathways are under systemic control and well-concerted together, adaptive mechanisms become triggered increasing systemic protection, activating antioxidant defense and repair machinery. Contextually, all attributes of mitochondrial patho-/physiology are instrumental for predictive medical approach and cost-effective treatments tailored to individualized patient profiles in primary (to protect vulnerable individuals again the health-to-disease transition) and secondary (to protect affected individuals again disease progression) care. Nutraceuticals are naturally occurring bioactive compounds demonstrating health-promoting, illness-preventing, and other health-related benefits. Keeping in mind health-promoting properties of nutraceuticals along with their great therapeutic potential and safety profile, there is a permanently growing demand on the application of mitochondria-relevant nutraceuticals. Application of nutraceuticals is beneficial only if meeting needs at individual level. Therefore, health risk assessment and creation of individualized patient profiles are of pivotal importance followed by adapted nutraceutical sets meeting individual needs. Based on the scientific evidence available for mitochondria-relevant nutraceuticals, this article presents examples of frequent medical conditions, which require protective measures targeted on mitochondria as a holistic approach following advanced concepts of predictive, preventive, and personalized medicine (PPPM/3PM) in primary and secondary care.

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“…10 µg mL -1 ), high lipophilicity (log p = 3.2), low chemical stability of its solutions, as well as low bioavailability (44%) with rapid metabolism. For these reasons, many research groups have been working to improve fisetin bioavailability by structure modification or by packing in various nanodelivery systems [40]. Such systems are based on the encapsulation of fisetin in nanoemulsions, liposomes, ethosomes, as well as in polymeric nanoparticles (for reviews, see [41][42][43][44]).…”

Section: Bioavailability Of Fisetinmentioning

confidence: 99%

Role of Fisetin in Selected Malignant Neoplasms in Women

Markowska,

Antoszczak,

Kacprzak

et al. 2023

Nutrients

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A promising therapeutic window and cost-effectiveness are just two of the potential advantages of using naturally derived drugs. Fisetin (3,3′,4′,7-tetrahydroxyflavone) is a natural flavonoid of the flavonol group, commonly found in fruit and vegetables. In recent years, fisetin has gained wide attention across the scientific community because of its broad spectrum of pharmacological properties, including cytotoxic activity against most abundant cancers. By stimulating or inhibiting selected molecular targets or biochemical processes, fisetin could affect the reduction of metastasis or cancer progression, which indicates its chemotherapeutic or chemopreventive role. In this review, we have summarized the results of studies on the anticancer effects of fisetin on selected female malignancies, both in in vitro and in vivo tests, i.e., breast, cervical, and ovarian cancer, published over the past two decades. Until now, no article dedicated exclusively to the action of fisetin on female malignancies has appeared. This review also describes a growing number of nanodelivery systems designed to improve the bioavailability and solubility of this natural compound. The reported low toxicity and activity of fisetin on cancer cells indicate its valuable potential, but large-scale clinical trials are urgently needed to assess real chemotherapeutic efficacy of this flavonoid.

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Fisetin—In Search of Better Bioavailability—From Macro to Nano Modifications: A Review

Cited by 17 publications

References 127 publications

A Fisetin Delivery System for Neuroprotection: A Co-Amorphous Dispersion Prepared in Supercritical Carbon Dioxide

A Fisetin Delivery System for Neuroprotection: A Co-Amorphous Dispersion Prepared in Supercritical Carbon Dioxide

Mini-encyclopedia of mitochondria-relevant nutraceuticals protecting health in primary and secondary care—clinically relevant 3PM innovation

Role of Fisetin in Selected Malignant Neoplasms in Women

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