Liposomal encapsulation of the natural flavonoid fisetin improves bioavailability and antitumor efficacy

Séguin, Johanne; Brullé, Laura; Boyer, Renaud; Lu, Yen Mei; Romano, Miriam; Touil, Yasmine; Scherman, Daniel; Bessodes, Michel; Mignet, Nathalie; Chabot, Guy G.

doi:10.1016/j.ijpharm.2013.01.050

Cited by 117 publications

(83 citation statements)

References 39 publications

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“…Unentrapped RES or RES-2-HPγCD inclusion complexes were separated from liposomes via size exclusion chromatography [25][26][27]. Briefly, two gel filtration columns were prepared with 3 mL equivalent of hydrated Sephadex G-50 and 0.2 mL of the formulation to be purified was added to each column.…”

Section: Determination Of Res Loading In the Liposomal Formulationsmentioning

confidence: 99%

Enhancing delivery and cytotoxicity of resveratrol through a dual nanoencapsulation approach

Soo

Thakur

et al. 2016

Journal of Colloid and Interface Science

107

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Despite the known anticancer potential of resveratrol, its clinical applications are often hindered by physicochemical limitations such as poor solubility and stability. The encapsulation of resveratrol in formulations such as polymeric nanoparticles and liposomes has shown limited success. This study aimed to develop and optimize a novel drug carrier by co-encapsulating pristine resveratrol alongside cyclodextrin-resveratrol inclusion complexes in the lipophilic and hydrophilic compartments of liposomes, respectively by using a novel dual carrier approach. The particle size, polydispersity index and zeta potential of the final formulation were 131±1.30nm, 0.089±0.005 and -2.64±0.51mV, respectively. Compared to free resveratrol and conventional liposomal formulations with drug release profile of 40-60%, our novel nanoformulations showed complete (100%) drug release in 24h. The formulation was stable for 14days at 4°C. We also studied the in vitro cytotoxicity of resveratrol encapsulated liposomes in HT-29 colon cancer cell lines. The cytotoxicity profile of our liposomes was observed to be dose dependent and enhanced in comparison to free resveratrol (in DMSO). Our study demonstrates that co-encapsulation of pristine resveratrol along with its cyclodextrin complex in liposomal formulations is a plausible option for the enhanced delivery of the hydrophobic chemotherapeutic agent.

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Section: Determination Of Res Loading In the Liposomal Formulationsmentioning

confidence: 99%

Enhancing delivery and cytotoxicity of resveratrol through a dual nanoencapsulation approach

Soo

Thakur

et al. 2016

Journal of Colloid and Interface Science

107

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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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“…Tea polyphenols, including EGCG, are also known for their limited bioavailability (Henning et al, 2005), although piperine has been shown to increase the bioavailability of EGCG in mice (Lambert et al, 2004). Liposomal encapsulation and nanoemulsion formulation enhanced the bioavailability and bioactivity of fisetin (Seguin et al, 2013;Ragelle et al, 2012). The bioavailability of galantamine in rats and mice administered by gavage was higher than that of galantamine administered with food (Monbaliu et al, 2003).…”

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confidence: 96%

Neuroprotective therapeutics from botanicals and phytochemicals against Huntington's disease and related neurodegenerative disorders

Dey

De²

2015

Journal of Herbal Medicine

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Liposomal encapsulation of the natural flavonoid fisetin improves bioavailability and antitumor efficacy

Cited by 117 publications

References 39 publications

Enhancing delivery and cytotoxicity of resveratrol through a dual nanoencapsulation approach

Enhancing delivery and cytotoxicity of resveratrol through a dual nanoencapsulation approach

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

Neuroprotective therapeutics from botanicals and phytochemicals against Huntington's disease and related neurodegenerative disorders

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