Physico-chemical characterization of inclusion complex between hydroxymethylnitrofurazone and hydroxypropyl-beta-cyclodextrin

Quimica nova

Grillo, Renato¹  Melo, Nathalie F. S. de¹  Fraceto, Leonardo Fernandes¹  Moraes, Carolina Morales²  Ferreira, Elizabeth Igne³  Brito, Charles L.³  Menezes, Carla M. S.³  Trossini, Gustavo H. G.³ 

[1] Universidade Estadual Paulista Júlio de Mesquita Filho, Sorocaba, Brasil;Universidade Estadual de Campinas, Campinas, Brasil;Universidade de São Paulo, São Paulo, Brasil

关键词: hydroxymethylnitrofurazone;    cyclodextrin;    inclusion complex.;   

DOI  :  10.1590/S0100-40422008000200019

学科分类：化学（综合）

来源: Sociedade Brasileira de Quimica

【 摘 要 】

Hydroxymethylnitrofurazone (NFOH) is a prodrugthat is active against Trypanosoma cruzi. It however presents low solubilityand high toxicity. Hydroxypropyl-b-cyclodextrin(HP-b-CD) can be used as a drug-delivery system forNFOH modifying its physico-chemical properties. The aim of this work is to characterizethe inclusion complex between NFOH and HP-b-CD. Therate of NFOH release decreases after complexation and thermodynamic parametersfrom the solubility isotherm studies revealed that a stable complex is formed(DGº= 1.7 kJ/mol). This study focuseson the physico-chemical characterization of a drug-delivery formulation thatcomes out as a potentially new therapeutic option for Chagas disease treatment.

【 授权许可】

CC BY