Formation of dendrimer-guest complexes as a strategy to increase the solubility of a phenazine N, N'-dioxide derivative with antitumor activity. Evaluation of PAMAM and PPI Dendrimers

DIB, NAHIR; OTERO, LUIS; BOSCH, PABLO; GONZÁLEZ, MERCEDES; SANTO, MARISA; LIAUDAT, ANA CECILIA; CERECETTO, HUGO; FERNÁNDEZ, LUCIANA; ALUSTIZA, FABRISIO; LAVAGGI, M. LAURA

Heliyon

Elsevier

Año: 2019 vol. 5

2405-8440

Poly(amidoamine) and Poly(propylenimine) dendrimers with different generationsand peripheral groups were studied as solubility enhancers and nanocarriers for7-bromo-2-hydroxy-phenazine N5,N10-dioxide. This compound possessespotential antitumoral and anti-trypanosomal activity, but its low solubility inphysiological media precludes its possible application as therapeutic drug. Theamino terminated dendrimers association with the active compounds as observedtrough NMR studies showed that electrostatic interactions are essential in thesolubilization enhancement process. The obtaining of a stable and no cytotoxicformulation makes the drug-carried association a suitable strategy for thegeneration of a drug delivery system for phenazine derivatives