Formation of dendrimer-guest complexes as a strategy to increase the solubility of a phenazine N, N′-dioxide derivative with antitumor activity
Poly(amidoamine) and Poly(propylenimine) dendrimers with different generations and peripheral groups were studied as solubility enhancers and nanocarriers for 7-bromo-2-hydroxy-phenazine N5,N10-dioxide. This compound possesses potential antitumoral and anti-trypanosomal activity, but its low solubil...
| Main Authors: | , , , , , , , , , |
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| Format: | Artículo |
| Language: | Inglés |
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Elsevier
2019
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| Online Access: | https://www.heliyon.com/article/e01528/ https://www.sciencedirect.com/science/article/pii/S2405844018337435 http://hdl.handle.net/20.500.12123/5019 https://doi.org/10.1016/j.heliyon.2019.e01528 |
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| author | Dib, Nahir Fernández, Luciana Santo, Marisa Otero, Luis Alustiza, Fabrisio Eduardo Liaudat, Ana Cecilia Bosch, Pablo Lavaggi, María Laura Cerecetto, Hugo González, Mercedes Florencia |
| author_browse | Alustiza, Fabrisio Eduardo Bosch, Pablo Cerecetto, Hugo Dib, Nahir Fernández, Luciana González, Mercedes Florencia Lavaggi, María Laura Liaudat, Ana Cecilia Otero, Luis Santo, Marisa |
| author_facet | Dib, Nahir Fernández, Luciana Santo, Marisa Otero, Luis Alustiza, Fabrisio Eduardo Liaudat, Ana Cecilia Bosch, Pablo Lavaggi, María Laura Cerecetto, Hugo González, Mercedes Florencia |
| author_sort | Dib, Nahir |
| collection | INTA Digital |
| description | Poly(amidoamine) and Poly(propylenimine) dendrimers with different generations and peripheral groups were studied as solubility enhancers and nanocarriers for 7-bromo-2-hydroxy-phenazine N5,N10-dioxide. This compound possesses potential antitumoral and anti-trypanosomal activity, but its low solubility in physiological media precludes its possible application as therapeutic drug. The amino terminated dendrimers association with the active compounds as observed trough NMR studies showed that electrostatic interactions are essential in the solubilization enhancement process. The obtaining of a stable and no cytotoxic formulation makes the drug-carried association a suitable strategy for the generation of a drug delivery system for phenazine derivatives. |
| format | Artículo |
| id | INTA5019 |
| institution | Instituto Nacional de Tecnología Agropecuaria (INTA -Argentina) |
| language | Inglés |
| publishDate | 2019 |
| publishDateRange | 2019 |
| publishDateSort | 2019 |
| publisher | Elsevier |
| publisherStr | Elsevier |
| record_format | dspace |
| spelling | INTA50192019-05-02T12:51:54Z Formation of dendrimer-guest complexes as a strategy to increase the solubility of a phenazine N, N′-dioxide derivative with antitumor activity Dib, Nahir Fernández, Luciana Santo, Marisa Otero, Luis Alustiza, Fabrisio Eduardo Liaudat, Ana Cecilia Bosch, Pablo Lavaggi, María Laura Cerecetto, Hugo González, Mercedes Florencia Bioquímica Nitrógeno Citotoxicidad Nanotecnología Biochemistry Nitrogen Cytotoxicity Nanotechnology Química Orgánica Poly(amidoamine) and Poly(propylenimine) dendrimers with different generations and peripheral groups were studied as solubility enhancers and nanocarriers for 7-bromo-2-hydroxy-phenazine N5,N10-dioxide. This compound possesses potential antitumoral and anti-trypanosomal activity, but its low solubility in physiological media precludes its possible application as therapeutic drug. The amino terminated dendrimers association with the active compounds as observed trough NMR studies showed that electrostatic interactions are essential in the solubilization enhancement process. The obtaining of a stable and no cytotoxic formulation makes the drug-carried association a suitable strategy for the generation of a drug delivery system for phenazine derivatives. EEA Marcos Juárez Fil: Dib, Nahir. Universidad Nacional de Río Cuarto. Departamento de Física y Departamento de Química; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina Fil: Fernández, Luciana. Universidad Nacional de Río Cuarto. Departamento de Física y Departamento de Química; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina Fil: Santo, Marisa. Universidad Nacional de Río Cuarto. Departamento de Física y Departamento de Química; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina Fil: Otero, Luis. Universidad Nacional de Río Cuarto. Departamento de Física y Departamento de Química; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina Fil: Alustiza, Fabrisio Eduardo. Instituto Nacional de Tecnología Agropecuaria (INTA). Estación Experimental Agropecuaria Marcos Juárez; Argentina Fil: Liaudat, Ana Cecilia. Universidad Nacional de Río Cuarto. Departamento de Biología Molecular; Argentina Fil: Bosch, Pablo. Universidad Nacional de Río Cuarto. Departamento de Biología Molecular; Argentina Fil: Lavaggi, María Laura. Universidad de la República. Facultad de Ciencias. Facultad de Química. Departamento de Química Orgánica; Uruguay Fil: Cerecetto, Hugo. Universidad de la República. Facultad de Ciencias. Facultad de Química. Departamento de Química Orgánica; Uruguay Fil: González, Mercedes Florencia. Universidad de la República. Facultad de Ciencias. Facultad de Química. Departamento de Química Orgánica; Uruguay 2019-05-02T12:49:41Z 2019-05-02T12:49:41Z 2019-04-23 info:ar-repo/semantics/artículo info:eu-repo/semantics/article info:eu-repo/semantics/publishedVersion https://www.heliyon.com/article/e01528/ https://www.sciencedirect.com/science/article/pii/S2405844018337435 http://hdl.handle.net/20.500.12123/5019 2405-8440 https://doi.org/10.1016/j.heliyon.2019.e01528 eng info:eu-repo/semantics/openAccess http://creativecommons.org/licenses/by-nc-sa/4.0/ Creative Commons Attribution-NonCommercial-ShareAlike 4.0 International (CC BY-NC-SA 4.0) application/pdf Elsevier Heliyon 5 (4) : e01528 (April 2019) |
| spellingShingle | Bioquímica Nitrógeno Citotoxicidad Nanotecnología Biochemistry Nitrogen Cytotoxicity Nanotechnology Química Orgánica Dib, Nahir Fernández, Luciana Santo, Marisa Otero, Luis Alustiza, Fabrisio Eduardo Liaudat, Ana Cecilia Bosch, Pablo Lavaggi, María Laura Cerecetto, Hugo González, Mercedes Florencia Formation of dendrimer-guest complexes as a strategy to increase the solubility of a phenazine N, N′-dioxide derivative with antitumor activity |
| title | Formation of dendrimer-guest complexes as a strategy to increase the solubility of a phenazine N, N′-dioxide derivative with antitumor activity |
| title_full | Formation of dendrimer-guest complexes as a strategy to increase the solubility of a phenazine N, N′-dioxide derivative with antitumor activity |
| title_fullStr | Formation of dendrimer-guest complexes as a strategy to increase the solubility of a phenazine N, N′-dioxide derivative with antitumor activity |
| title_full_unstemmed | Formation of dendrimer-guest complexes as a strategy to increase the solubility of a phenazine N, N′-dioxide derivative with antitumor activity |
| title_short | Formation of dendrimer-guest complexes as a strategy to increase the solubility of a phenazine N, N′-dioxide derivative with antitumor activity |
| title_sort | formation of dendrimer guest complexes as a strategy to increase the solubility of a phenazine n n dioxide derivative with antitumor activity |
| topic | Bioquímica Nitrógeno Citotoxicidad Nanotecnología Biochemistry Nitrogen Cytotoxicity Nanotechnology Química Orgánica |
| url | https://www.heliyon.com/article/e01528/ https://www.sciencedirect.com/science/article/pii/S2405844018337435 http://hdl.handle.net/20.500.12123/5019 https://doi.org/10.1016/j.heliyon.2019.e01528 |
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