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Campo DC | Valor | Lengua/Idioma |
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dc.contributor.author | Lecot Calandria, Nicole Valerie | - |
dc.contributor.author | Dávila Saralegui, Belén | - |
dc.contributor.author | Sánchez, Carina | - |
dc.contributor.author | Fernández Lomonaco, Marcelo Luis | - |
dc.contributor.author | González, Mercedes | - |
dc.contributor.author | Cabral González, Pablo | - |
dc.contributor.author | Cerecetto, Hugo | - |
dc.date.accessioned | 2023-11-22T14:39:10Z | - |
dc.date.available | 2023-11-22T14:39:10Z | - |
dc.date.issued | 2022 | - |
dc.identifier.citation | Lecot Calandria, N, Dávila Saralegui, B, Sánchez, C, [y otros autores]. "Development and evaluation of 2-amino-7-fluorophenazine 5,10-dioxide polymeric micelles as antitumoral agents for 4T1 breast cancer". Polymers. [en línea] 2022, 14(1): 71. 14 h. | es |
dc.identifier.issn | 2073-4360 | - |
dc.identifier.uri | https://hdl.handle.net/20.500.12008/41421 | - |
dc.description.abstract | 2-Amino-7-fluorophenazine 5,10-dioxide (FNZ) is a bioreducible prodrug, poorly soluble in water, with potential anticancer activity on hypoxic-tumors. This poor solubility limits its potential applications in clinic. Amphiphilic pristine polymeric micelles (PMs) based on triblock copolymers Pluronic® and Tetronic®, glycosylated derivatives and their mixtures with preformed-liposomes (LPS), were analyzed as strategies to improve the bioavailability of FNZ. FNZ encapsulations were performed and the obtaining nanostructures were characterized using UV-visible spectroscopy (UV-VIS), Transmission Electron Microscopy (TEM) and Dynamic Light Scattering (DLS). The most promising nanoformulations were analyzed for their potential toxicity and pharmacologically, at 20 mg/kg FNZ-doses, in a stage-IV murine metastatic-breast tumor model. The results revealed that the solubility of the encapsulated-FNZ increased up to 14 times and the analysis (UV-VIS, DLS and TEM) confirmed the interaction between vehicles and FNZ. In all the cases appropriate encapsulation efficiencies (greater than 75%), monodisperse nanometric particle sizes (PDI = 0.180–0.335), adequate Z-potentials (−1.59 to −26.4 mV), stabilities and spherical morphologies were obtained. The in vitro profile of FNZ controlled releases corresponded mainly to a kinetic Higuchi model. The in vitro/in vivo biological studies revealed non-toxicity and relevant tumor-weight diminution (up to 61%). | es |
dc.description.sponsorship | ANII: FCE_1_2014_1_104714 | es |
dc.description.sponsorship | ANII: POS_FCE_2015_1_1005193 | es |
dc.format.extent | 14 h. | es |
dc.format.mimetype | application/pdf | es |
dc.language.iso | en_US | es |
dc.publisher | MDPI | es |
dc.relation.ispartof | Polymers, 2022, 14(1): 71. | es |
dc.rights | Las obras depositadas en el Repositorio se rigen por la Ordenanza de los Derechos de la Propiedad Intelectual de la Universidad de la República.(Res. Nº 91 de C.D.C. de 8/III/1994 – D.O. 7/IV/1994) y por la Ordenanza del Repositorio Abierto de la Universidad de la República (Res. Nº 16 de C.D.C. de 07/10/2014) | es |
dc.subject | Bioreductive-drug | es |
dc.subject | Phenazine-5,10-dioxide | es |
dc.subject | Amphiphilic pristine polymeric micelles | es |
dc.subject | 4T1-tumor mode | es |
dc.subject | In vivo antitumoral activity | es |
dc.title | Development and evaluation of 2-amino-7-fluorophenazine 5,10-dioxide polymeric micelles as antitumoral agents for 4T1 breast cancer | es |
dc.type | Artículo | es |
dc.contributor.filiacion | Lecot Calandria Nicole Valerie, Universidad de la República (Uruguay). Facultad de Ciencias. Centro de Investigaciones Nucleares. | - |
dc.contributor.filiacion | Dávila Saralegui Belén, Universidad de la República (Uruguay). Facultad de Ciencias. Instituto de Química Biológica. | - |
dc.contributor.filiacion | Sánchez Carina, Universidad de la República (Uruguay). Facultad de Ciencias. Instituto de Química Biológica. | - |
dc.contributor.filiacion | Fernández Lomonaco Marcelo Luis, Universidad de la República (Uruguay). Facultad de Ciencias. Centro de Investigaciones Nucleares. | - |
dc.contributor.filiacion | González Mercedes, Universidad de la República (Uruguay). Facultad de Ciencias. Instituto de Química Biológica. | - |
dc.contributor.filiacion | Cabral González Pablo, Universidad de la República (Uruguay). Facultad de Ciencias. Centro de Investigaciones Nucleares. | - |
dc.contributor.filiacion | Cerecetto Hugo, Universidad de la República (Uruguay). Facultad de Ciencias. Instituto de Química Biológica. | - |
dc.rights.licence | Licencia Creative Commons Atribución (CC - By 4.0) | es |
dc.identifier.doi | 10.3390/polym14010071 | - |
Aparece en las colecciones: | Publicaciones académicas y científicas - Facultad de Ciencias |
Ficheros en este ítem:
Fichero | Descripción | Tamaño | Formato | ||
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103390polym14010071.pdf | 2,2 MB | Adobe PDF | Visualizar/Abrir |
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