Study of the interaction between hydroxymethylnitrofurazone and 2-hydroxypropyl-beta-cyclodextrin.

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作者：

R Grillo，NFSD Melo，CM Moraes，RD Lima，CMS Menezes，EI Ferreira，AH Rosa，LF Fraceto

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摘要：

Chagas disease is a serious health problem in Latin America. Hidroxymethylnitrofurazone (NFOH) is a nitrofurazone prodrug more active than nitrofurazone against column, using acetonitrile–water (20/80, v/v) as the mobile phase, in which HP-β-CD was incorporated as a mobile phase additive. The decrease in the retention times with increasing concentrations of HP-β-CD enables the determination of the apparent stability constant of the complex (=6.2±0.3M) by HPLC. The solubility isotherm was studied and the value for the apparent stability constant (=7.9±0.2M) was calculated. The application of continuous variation method indicated the presence of a complex with 1:1 NFOH:HP-β-CD stoichiometry. The photostability study showed that the formation of an inclusion complex had a destabilizing effect on the photodecomposition of NFOH when compared to that of the "free" molecule in solution. The mobility investigation (by NMR longitudinal relaxation time) gives information about the complexation of NFOH with HP-β-CD. In preliminary toxicity studies, cell viability tests revealed that inclusion complexes were able to decrease the toxic effect (

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关键词：

2-Hydroxypropyl-β-cyclodextrin Solubility isotherm Nuclear magnetic resonance Toxicity

DOI：

10.1016/j.jpba.2008.01.010

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年份：

2008