Designing fisetin nanocrystals for enhanced in cellulo anti-angiogenic and anticancer efficacy

Ma, Panpan; Séguin, Johanne; Ly, Ky-Nhu; Henríquez, Luis Castillo; Plansart, Eva; Hammad, Karim; Gahoual, Rabah; Dhôtel, Hélène; Izabelle, Charlotte; Saubaméa, Bruno; Richard, Cyrille; Escriou, Virginie; Mignet, Nathalie; Corvis, Yohann

doi:10.1016/j.ijpx.2022.100138

Cited by 9 publications

(14 citation statements)

References 84 publications

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“…The characteristic absorption bands of FIS raw powder appear at 808 cm −1 (out-ofplane C-H bending), 934 cm −1 (C-C-C bending), 972 cm −1 (C-C-C-H torsion), 1101 cm −1 (C-O stretching), 1117 cm −1 (C-OH stretching), 1163 cm −1 (C-OH stretching), 1329 cm −1 (C-OH deformation), 1522 cm −1 (C-C stretching), 1566 cm −1 (C-C stretching), 1599 cm −1 (aromatic ring vibration), 3246 cm −1 and 3346 cm −1 (OH stretching of the hydroxyl groups), 3518 cm −1 and 3553 cm −1 (stretching vibrations of phenolic O-H bonds) [52][53][54][55].…”

Section: Resultsmentioning

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: Resultsmentioning

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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“…However, the obstacles to drug delivery come in different forms and involve poor biopharmaceutical properties of the APIs such as chemical instability, low solubility, low permeability, and rapid metabolism and elimination from the body [123] . To overcome the mentioned barriers, numerous APIs are formulated as nanocrystals or encapsulated in different types of drug delivery systems, such as polymeric nanoparticles [124–126] . In the following sections, we highlight the interest of using TheDESs as solvents of APIs or as the active compound itself to improve their bioavailability.…”

Section: Role Of Deep Eutectic Solvents In Drug Engineeringmentioning

confidence: 99%

“…[123] To overcome the mentioned barriers, numerous APIs are formulated as nanocrystals or encapsulated in different types of drug delivery systems, such as polymeric nanoparticles. [124][125][126] In the following sections, we highlight the interest of using TheDESs as solvents of APIs or as the active compound itself to improve their bioavailability. We also illustrate the involvement of DESs as reaction media or catalysts for the synthesis of various APIs.…”

Section: Role Of Deep Eutectic Solvents In Drug Engineeringmentioning

confidence: 99%

Deep Eutectic Solvents: An Eco‐friendly Design for Drug Engineering

et al. 2023

Self Cite

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In the spirit of circular economy and sustainable chemistry, the use of environmentally friendly chemical products in pharmacy has become a hot topic. In recent years, organic solvents have been the subject of a great range of restriction policies due to their harmful effects on the environment and toxicity to human health. In parallel, deep eutectic solvents (DESs) have emerged as suitable greener solvents with beneficial environmental impacts and a rich palette of physico‐chemical advantages related to their low cost and biocompatibility. Additionally, DESs can be accompanied by a remarkable solubilizing effect for several active pharmaceutical ingredients (APIs), thus forming therapeutic DESs (TheDESs). In this work, special attention is paid to DESs, presenting a precise definition, classification, methods of preparation, and characterization. A description of natural DESs (NaDESs), i.e., eutectic solvents present in natural sources, is also reported. Moreover, the present review article is the first one to detail the different approaches for judiciously selecting the constituents of DESs in order to minimize the number of experiments. The role of DESs in the biomedical and pharmaceutical sectors and their impact on the development of successful therapies are also discussed.

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“…Morphological studies confirmed an increase in the apoptosis of the endothelial cells as well as an improved anti-angiogenic effect of fisetin nanocrystals. The nanosuspension with fisetin was also stable after adding cryoprotectant for 120 and 30 days at −80 °C and 5 °C, respectively [ 101 ].…”

Section: Nanocrystalsmentioning

confidence: 99%

“…This suggests that using polymeric micelles could be a successful option for fisetin’s carrier in the battle against breast cancer. On the other hand, fisetin nanocrystals demonstrated maximum cytotoxicity when tested against Lewis lung cancer cells in vitro [ 101 ]. In vivo studies showed that fisetin nanoemulsion reduced tumor size and, when incorporated into liposomes (DOPC, DODA-PEG 2000 ), delayed tumor growth [ 49 , 87 ].…”

Section: Comparison Of the Effects Of Fisetin Pre-formulation Modific...mentioning

confidence: 99%

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

Szymczak,

Cielecka-Piontek

2023

IJMS

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As secondary plant metabolites, polyphenols are abundant in fruits and vegetables. They are in high demand because of their many health benefits. However, their low bioavailability makes them complex compounds to use for therapeutic purposes. Due to the limited solubility of phytocompounds, dietary supplements made from them may only be partially effective. Such molecules include fisetin, found in strawberries, and have shown great promise in treating Alzheimer’s disease and cancer. Unfortunately, because of their limited water solubility, low absorption, and poor bioavailability, the assistance of nanotechnology is required to allow them to fulfil their potential fully. Here, we provide evidence that nanodelivery methods and structure modifications can improve fisetin bioavailability, which is linked to improvements in therapeutic efficacy. An open question remains as to which nanocarrier should be chosen to meet the abovementioned requirements and be able to enhance fisetin’s therapeutic potential to treat a particular disease.

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Designing fisetin nanocrystals for enhanced in cellulo anti-angiogenic and anticancer efficacy

Cited by 9 publications

References 84 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

Deep Eutectic Solvents: An Eco‐friendly Design for Drug Engineering

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

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