Fisetin-loaded nanocochleates: formulation, characterisation,<i>in vitro</i>anticancer testing, bioavailability and biodistribution study

Bothiraja, C.; Yojana, Bhagwat D; Pawar, Atmaram; Shaikh, Karimunnisa S.; Thorat, Uday H

doi:10.1517/17425247.2013.860131

Cited by 79 publications

(70 citation statements)

References 42 publications

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“…Bothiraja et al [12] examined the bioavailability of fisetin-loaded nanocochelates which are lipid-based supramolecular assemblies containing negatively charged phospholipid and a divalent cation. Pharmacokinetic studies in mice showed that there was a sustained release of fisetin at physiological pH and when nanocochleates were administered ip, there was low tissue distribution and massive increase (141-fold) in relative bioavailability [12].…”

Section: Bioavailability and Pharmacokinetics Of Fisetinmentioning

confidence: 99%

Exploring the molecular targets of dietary flavonoid fisetin in cancer

Syed

Adhami

Khan

et al. 2016

Seminars in Cancer Biology

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The last few decades have seen a resurgence of interest among the scientific community in exploring the efficacy of natural compounds against various human cancers. Compounds of plant origin belonging to different groups such as alkaloids, flavonoids and polyphenols evaluated for their cancer preventive effects have yielded promising data, thereby offering a potential therapeutic alternative against this deadly disease. The flavonol fisetin (3,3′,4′,7-tetrahydroxyflavone), present in fruits and vegetables such as strawberries, apple, cucumber, persimmon, grape and onion, was shown to possess anti-microbial, anti-inflammatory, anti-oxidant and more significantly anti-carcinogenic activity when assessed in diverse cell culture and animal model systems. The purpose of this review is to update and discuss key findings obtained till date from in vitro and in vivo studies on fisetin, with special focus on its anti-cancer role. The molecular mechanism(s) described in the observed growth inhibitory effects of fisetin in different cancer cell types is also summarized. Moreover, an attempt is made to analyze the direction required for future studies that could lead to the development of fisetin as a potent chemopreventive/chemotherapeutic agent against cancer.

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Section: Bioavailability and Pharmacokinetics Of Fisetinmentioning

confidence: 99%

Exploring the molecular targets of dietary flavonoid fisetin in cancer

Syed

Adhami

Khan

et al. 2016

Seminars in Cancer Biology

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“…Previously, attempts have been made for the delivery of FST using lipid-based carriers and chelating agents such as calcium (Bothiraja et al, 2014). However, these attempts were limited to intraperitoneal and intravenous administration only.…”

Section: Introductionmentioning

confidence: 99%

Enhanced oral bioavailability and anticancer efficacy of fisetin by encapsulating as inclusion complex with HPβCD in polymeric nanoparticles

et al. 2017

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Fisetin (FST), a potent anticancer phytoconstituent, exhibits poor aqueous solubility and hence poor bioavailability. The aim of the present study is to improve the oral bioavailability of FST by encapsulating into PLGA NPs (poly-lactide-co-glycolic acid nanoparticles) as a complex of HPbCD (hydroxyl propyl beta cyclodextrin) and to assess its anti-cancer activity against breast cancer cells. FST-HPbCD inclusion complex (FHIC) was prepared and the supramolecular complex formation was characterized by FTIR, DSC, PXRD and 1 H NMR. FHIC encapsulated PLGA nanoparticles (FHIC-PNP) were prepared and were studied for in vitro anticancer activity, cellular uptake, apoptosis and reactive oxygen species generation in MCF-7 human breast cancer cells. Comparative bioavailability of FST was determined after oral administration in C57BL6 mice as pure FST and FHIC-PNP. The results revealed that FHIC-PNP not only enhanced the anti-cancer activity and apoptosis of FST against MCF-7 cells but also improved its oral bioavailability, as demonstrated by increased peak plasma concentration and total drug absorbed.

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“…Fisetin has been formulated in nanoemulsions [6], nanocochleates [7], liposomes [8,9] and cyclosophoroase dimer complexes [10].…”

Section: Introductionmentioning

confidence: 99%

Design and development of dry powder sulfobutylether-β-cyclodextrin complex for pulmonary delivery of fisetin

Mohtar

Taylor

Sheikh

et al. 2017

European Journal of Pharmaceutics and Biopharmaceutics

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This study has investigated complexation of fisetin, a natural flavonoid, with three types of cyclodextrins to improve its solubility. Sulfobutylether-β-cyclodextrin (SBE-β-CD) showed the highest complexation efficiency while maintaining the in vitro antioxidant activity of fisetin. Addition of 20 %v/v ethanol in water improved the amount of solubilized fisetin in the complex 5.9-fold compared to the system containing water alone. Spray drying of fisetin-SBE-β-CD complex solution in the presence of ethanol produced a dry powder with improved aerosolization properties when delivered from a dry powder inhaler, indicated by a 2-fold increase in the fine particle fraction (FPF) compared to the powder produced from the complex solution containing water alone. The pitted morphological surface of these particles suggested a more hollow internal structure, indicating a lighter and less dense powder.Incorporation of 20 %w/w leucine improved the particle size distribution of the powder and further increased the FPF by 2.3-fold. This formulation also showed an EC 50 value equivalent to fisetin alone in the A549 cell line. In conclusion, an inhalable dry powder containing fisetin-SBE-β-CD complex was successfully engineered with an improved aqueous solubility of fisetin. The dry powder may be useful to deliver high amounts of fisetin to the deep lung region for therapeutic purposes. KEYWORDSFisetin, sulfobutylether-β-cyclodextrin, pulmonary delivery, spray drying, leucine, A549 cell line.

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Fisetin-loaded nanocochleates: formulation, characterisation,in vitroanticancer testing, bioavailability and biodistribution study

Cited by 79 publications

References 42 publications

Exploring the molecular targets of dietary flavonoid fisetin in cancer

Exploring the molecular targets of dietary flavonoid fisetin in cancer

Enhanced oral bioavailability and anticancer efficacy of fisetin by encapsulating as inclusion complex with HPβCD in polymeric nanoparticles

Design and development of dry powder sulfobutylether-β-cyclodextrin complex for pulmonary delivery of fisetin

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