Formation of dendrimer-guest complexes as a strategy to increase the solubility of a phenazine N, N'-dioxide derivative with antitumor activity

树枝状聚合物-客体复合物的形成作为增加具有抗肿瘤活性的吩嗪 N,N'-二氧化物衍生物溶解度的策略

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作者:Nahir Dib, Luciana Fernández, Marisa Santo, Luis Otero, Fabrisio Alustiza, Ana Cecilia Liaudat, Pablo Bosch, M Laura Lavaggi, Hugo Cerecetto, Mercedes González

Abstract

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 N 5,N 10-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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