Química Nova (Jan 2008)

Caracterização físico-química de complexo de inclusão entre hidroximetilnitrofurazona e hidroxipropil-beta-ciclodextrina Physico-chemical characterization of inclusion complex between hydroxymethylnitrofurazone and hydroxypropyl-beta-cyclodextrin

  • Renato Grillo,
  • Nathalie F. S. de Melo,
  • Leonardo Fernandes Fraceto,
  • Charles L. Brito,
  • Gustavo H. G. Trossini,
  • Carla M. S. Menezes,
  • Elizabeth Igne Ferreira,
  • Carolina Morales Moraes

DOI
https://doi.org/10.1590/S0100-40422008000200019
Journal volume & issue
Vol. 31, no. 2
pp. 290 – 295

Abstract

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Hydroxymethylnitrofurazone (NFOH) is a prodrug that is active against Trypanosoma cruzi. It however presents low solubility and high toxicity. Hydroxypropyl-beta-cyclodextrin (HP-beta-CD) can be used as a drug-delivery system for NFOH modifying its physico-chemical properties. The aim of this work is to characterize the inclusion complex between NFOH and HP-beta-CD. The rate of NFOH release decreases after complexation and thermodynamic parameters from the solubility isotherm studies revealed that a stable complex is formed (deltaGº= 1.7 kJ/mol). This study focuses on the physico-chemical characterization of a drug-delivery formulation that comes out as a potentially new therapeutic option for Chagas disease treatment.

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