The DOI matches its Crossref record; 2 of the 2 references it cites were found in a registry or an index.
Nanoemulsion formulation of fisetin improves bioavailability and antitumour activity in mice
Open accessAbstract
The natural flavonoid fisetin (3,3',4',7-tetrahydroxyflavone) has shown antitumour activity but its administration is complicated by its low water solubility. Our aim was to incorporate fisetin into a nanoemulsion to improve its pharmacokinetics and therapeutic efficacy. Solubility and emulsification tests allowed to develop an optimal nanoemulsion composed of Miglyol 812N/Labrasol/Tween 80/Lipoid E80/water (10%/10%/2.5%/1.2%/76.3%). The nanoemulsion had an oil droplet diameter of 153 ± 2 nm, a negative zeta potential (-28.4 ± 0.6 mV) and a polydispersity index of 0.129. The nanoemulsion was stable at 4 °C for 30 days, but phase separation occurred at 20 °C. Pharmacokinetic studies in mice revealed that the fisetin nanoemulsion injected intravenously (13 mg/kg) showed no significant difference in systemic exposure compared to free fisetin. However, when the fisetin nanoemulsion was administered intraperitoneally, a 24-fold increase in fisetin relative bioavailability was noted, compared to free fisetin. Additionally, the antitumour activity of the fisetin nanoemulsion in Lewis lung carcinoma bearing mice occurred at lower doses (36.6 mg/kg) compared to free fisetin (223 mg/kg). In conclusion, we have developed a stable nanoemulsion of fisetin and have shown that it could improve its relative bioavailability and antitumour activity.
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Cites
Cancer chemoprevention with dietary phytochemicals
Surh, Y.-J. (2003) · Nature reviews. Cancer · doi:10.1038/nrc1189 · Cited by 2,955
Engineering of nanoemulsions for drug delivery
Sarker, D. (2005) · Current Drug Delivery · doi:10.2174/156720105774370267 · Cited by 268 · cited 1×
“Nanoemulsions represent good vehicles to formulate hydrophobic active molecules (Sarker, 2005). ep Finally, the antitumour activity of the fisetin nanoemulsion was compared to the administration of free fisetin in Lewis lung carcinoma bearing mice.”
Cited by
Nanoemulsion: Concepts, development and applications in drug delivery
Singh, Y., Meher, J. G., Raval, K., Khan, F. A., Chaurasia, M., Jain, N. K., & Chourasia, M. K. (2017) · Journal of Controlled Release · doi:10.1016/j.jconrel.2017.03.008 · Cited by 1,358
Intraperitoneal Route of Drug Administration: Should it Be Used in Experimental Animal Studies?
Al Shoyaib, A., Archie, S. R., & Karamyan, V. T. (2020) · Pharmaceutical Research · doi:10.1007/s11095-019-2745-x · Cited by 631
Techniques for Formulation of Nanoemulsion Drug Delivery System: A Review
Kumar, M., Bishnoi, R. S., Shukla, A. K., & Jain, C. P. (2019) · Preventive Nutrition and Food Science · doi:10.3746/pnf.2019.24.3.225 · Cited by 441
Senolytics reduce coronavirus-related mortality in old mice
Camell, C. D., Yousefzadeh, M. J., Zhu, Y., Prata, L. G. P. L., Huggins, M. A., Pierson, M., Zhang, L., O’Kelly, R. D., Pirtskhalava, T., Xun, P., et al. (2021) · Science · doi:10.1126/science.abe4832 · Cited by 320
Sivakumar, M., Tang, S. Y., & Tan, K. W. (2014) · Ultrasonics Sonochemistry · doi:10.1016/j.ultsonch.2014.03.025 · Cited by 279
Metadata
- Authors
- Ragelle, H., Crauste-Manciet, S., Seguin, J., Brossard, D., Scherman, D., Arnaud, P., & Chabot, G. G.
- Venue
- International Journal of Pharmaceutics
- Publisher
- Elsevier BV
- Published
- 2012-05
- Volume
- 427
- Issue
- 2
- Pages
- 452-459
- ISSN
- 0378-5173 (ISSN-L)
- OpenAlex
- W2141217262
- Cited by
- 213
- References
- 2
- FWCI
- 7.54
- Type
- journal article
- Language
- en
- Open access
- green
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- Ragelle, H., Crauste-Manciet, S., Seguin, J., Brossard, D., Scherman, D., Arnaud, P., & Chabot, G. G. (2012). Nanoemulsion formulation of fisetin improves bioavailability and antitumour activity in mice. International Journal of Pharmaceutics. https://doi.org/10.1016/j.ijpharm.2012.02.025
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Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).
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