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(Referência obtida automaticamente do Web of Science, por meio da informação sobre o financiamento pela FAPESP e o número do processo correspondente, incluída na publicação pelos autores.)

Hydroxymethylnitrofurazone:Dimethyl-beta-cyclodextrin Inclusion Complex: A Physical-Chemistry Characterization

Texto completo
Autor(es):
Grillo, Renato [1] ; Silva Melo, Nathalie Ferreira [1] ; Moraes, Carolina Morales [2] ; Rosa, Andre Henrique [1] ; Frutuoso Roveda, Jose Arnaldo [1] ; Menezes, Carla M. S. [3] ; Ferreira, Elizabeth Igne [3] ; Fraceto, Leonardo Fernandes [2, 1]
Número total de Autores: 8
Afiliação do(s) autor(es):
[1] State Univ Sao Paulo, Dept Environm Engn, BR-18087180 Sorocaba, SP - Brazil
[2] Univ Estadual Campinas, Inst Biol, Dept Biochem, Campinas, SP - Brazil
[3] Univ Sao Paulo, Fac Pharmaceut Sci, LAPEN, Sao Paulo - Brazil
Número total de Afiliações: 3
Tipo de documento: Artigo Científico
Fonte: Journal of Biological Physics; v. 33, n. 5-6, p. 445-453, DEC 2007.
Citações Web of Science: 12
Resumo

Hydroxymethylnitrofurazone (NFOH) is active against Trypanosoma cruzi; however, its low solubility and high toxicity precludes its current use in treatment of parasitosis. Cyclodextrin can be used as a drug carrier system, as it is able to form inclusion (host-guest) complexes with a wide variety of organic (guest) molecules. Several reports have shown the interesting use of modified beta-cyclodextrins in pharmaceutical formulation, to improve the bioavailability of drugs and to decrease their toxicity. The aim of this work was to characterize inclusion complexes formed between NFOH and dimethyl-beta-cyclodextrin (DM-beta-CD) by complexation/release kinetics and solubility isotherm experiments using ultraviolet (UV)-visible spectrophotometry and by the measurement of the dynamics information obtained from T (1) relaxation times and diffusion (DOSY) experiments using nuclear magnetic resonance (NMR) spectroscopy. The complex was prepared at different NFOH and DM-beta-CD molar ratios. The UV-visible measurements were recorded in a spectrophotometer, and NMR experiments were recorded at 20 degrees C on a NMR spectrometer (Varian Inova) operating at 500 MHz. Longitudinal relaxation times were obtained by the conventional inversion-recovery method and the DOSY experiments were carried out using the BPPSTE sequence. The kinetics of complexation revealed that 30 h is enough for stabilization of the NFOH absorbance in presence of cyclodextrin. Solubility isotherm studies show a favorable complexation and increase in solubility when NFOH interacts with cyclodextrin. The analysis of the NMR-derived diffusion coefficients and T (1) relaxation times shows that in the presence of DM-beta-CD, NFOH decreases its mobility in solution, indicating that this antichagasic compound interacts with the cyclodextrin cavity. The release kinetics assays showed that NFOH changes its release profile when in the presence of cyclodextrin due to complexation. This study was focused on the physicochemical characterization of drug-delivery formulations that may serve as potentially new therapeutic options for the treatment of Chagas' disease. (AU)

Processo FAPESP: 04/02091-4 - Caracterização físico-química de complexo de S(-) bupivacaína em ciclodextrinas desenvolvido para o tratamento da dor
Beneficiário:Carolina Morales Moraes
Linha de fomento: Bolsas no Brasil - Iniciação Científica
Processo FAPESP: 05/03045-9 - Preparo e caracterização de complexos de inclusão entre compostos antichagásicos e ciclodextrinas
Beneficiário:Leonardo Fernandes Fraceto
Linha de fomento: Auxílio à Pesquisa - Regular
Processo FAPESP: 06/00787-7 - Preparo e caracterização de complexos de inclusão entre hidroximetil nitrofural e ciclodextrinas
Beneficiário:Renato Grillo
Linha de fomento: Bolsas no Brasil - Iniciação Científica