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Formation of dendrimer-guest complexes as a strategy to increase the solubility of a phenazine N, N′-dioxide derivative with antitumor activity
Resumen
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
[ver mas...]
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.
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Autor
Dib, Nahir;
Fernández, Luciana;
Santo, Marisa;
Otero, Luis;
Alustiza, Fabrisio Eduardo;
Liaudat, Ana Cecilia;
Bosch, Pablo;
Lavaggi, María Laura;
Cerecetto, Hugo;
González, Mercedes Florencia;
Fuente
Heliyon 5 (4) : e01528 (April 2019)
Fecha
2019-04-23
Editorial
Elsevier
ISSN
2405-8440
Formato
pdf
Tipo de documento
artículo
Palabras Claves
Derechos de acceso
Abierto
Excepto donde se diga explicitamente, este item se publica bajo la siguiente descripción: Creative Commons Attribution-NonCommercial-ShareAlike 2.5 Unported (CC BY-NC-SA 2.5)