Academic Journal
Fisetin-Loaded Nanostructured Lipid Carriers: Formulation and Evaluations against Advanced and Metastatic Melanoma
| العنوان: | Fisetin-Loaded Nanostructured Lipid Carriers: Formulation and Evaluations against Advanced and Metastatic Melanoma |
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| المؤلفون: | Hitesh Kumar, Pallavi Chand, Shantanu Pachal, Sahid Mallick, Rupshee Jain, SubbaRao V. Madhunapantula, Vikas Jain |
| سنة النشر: | 2023 |
| مصطلحات موضوعية: | Biophysics, Biochemistry, Cell Biology, Molecular Biology, Pharmacology, Biotechnology, Developmental Biology, Cancer, Biological Sciences not elsewhere classified, Chemical Sciences not elsewhere classified, nanostructured lipid carriers, fold higher inhibition, fold higher compared, demonstrated sustained release, 79 ± 3, studies demonstrated 5, b16f10 cells compared, 16 ± 1, least ∼ 3, 176 ± 0, study demonstrated fis, optimized nlcs depict, bax mrna expression, 0 ± 5, 50 , metastatic melanoma fisetin, ∼ 1, 5 nm, vivo <, metastatic melanoma |
| الوصف: | Fisetin (Fis), a natural flavonoid with anticancer effects, suffers from delivery constraints. Fisetin-nanostructured lipid carriers (NLCs) were developed for better efficacy against metastatic melanoma, employing the design of experiment (DoE) approach. The optimized NLCs depict a particle diameter of 135.0 ± 5.5 nm, a polydispersity index (PDI) of 0.176 ± 0.035, and an entrapment efficiency of 78.16 ± 1.58%. The formulation was stable over a period of 60 days and demonstrated sustained release of the drug (74.79 ± 3.75%) over 96 h. Fis-NLCs depicted at least ∼3.2 times lower IC 50 value and ∼1.8 times higher drug uptake at 48 h in A-375 and B16F10 cells compared to that of Fis. It also inhibited the mobility of melanoma cells and induced cell cycle arrest at the G1/S phase. Reverse transcriptase polymerase chain reaction (RT-PCR) and Western blot results show enhanced expression of Nrf2/NQO1 genes and an apoptotic effect by the upregulation of BAX mRNA expression. The protein levels of BAX and p53 were ∼2-fold higher compared with that of pure Fis. In-vivo studies demonstrated 5.9- and 10.7-fold higher inhibition in melanoma-associated metastasis in the lungs and liver, respectively. The outcomes from this study demonstrated Fis-NLCs as an effective tool against melanoma. |
| نوع الوثيقة: | article in journal/newspaper |
| اللغة: | unknown |
| Relation: | https://figshare.com/articles/journal_contribution/Fisetin-Loaded_Nanostructured_Lipid_Carriers_Formulation_and_Evaluations_against_Advanced_and_Metastatic_Melanoma/24469948 |
| DOI: | 10.1021/acs.molpharmaceut.3c00309.s001 |
| الاتاحة: | https://doi.org/10.1021/acs.molpharmaceut.3c00309.s001 https://figshare.com/articles/journal_contribution/Fisetin-Loaded_Nanostructured_Lipid_Carriers_Formulation_and_Evaluations_against_Advanced_and_Metastatic_Melanoma/24469948 |
| Rights: | CC BY-NC 4.0 |
| رقم الانضمام: | edsbas.70350B71 |
| قاعدة البيانات: | BASE |
| DOI: | 10.1021/acs.molpharmaceut.3c00309.s001 |
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