Alternativas para o tratamento da esquistossomose: Caracterizacao fisico-quimica do complexo de inclusao entre praziquantel e hidroxipropil-β-ciclodextrina
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Data
2010-12-01
Autores
Chaves, Izabel S.
Rodrigues, Stella G.
Melo, Nathalie F.S. [UNESP]
de Jesus, Marcelo B.
Fraceto, Leonardo F. [UNESP]
de Paula, Eneida
Pinto, Luciana M.A.
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Resumo
Praziquantel (PZQ) is the drug of choice commonly used for the treatment of shistosomiasis. However, it has low aqueous solubility, which could limit its bioavailability in the body. To circumvent these features, an inclusion complex with hydroxypropyl-beta- cyclodextrin (HP-β-CD) was prepared. Thus, the objective of this work was to prepare and characterize the PZQ/HP-β-CD inclusion complex. Morphological, spectroscopic, and calorimetric analysis showed the first signs of the guest/host interaction. The complexation kinetic analysis was used to determine the kinetic constant and, besides that, it was possible to establish the time consumed to reach equilibrium. Using the solubility isotherm, it was observed that the interaction with HP-β-CD increased 2.4 fold the aqueous solubility of plain PZQ. In vitro cytotoxicity tests, using fibroblast cells, evidenced no toxicity for these cells at the concentrations tested. These results demonstrated that there is a potential use of PZQ in formulations with HP-β-CD.
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Cyclodextrin, Inclusion complex, Praziquantel, Schistosomiasis, 2 hydroxypropyl beta cyclodextrin, praziquantel, calorimetry, chemical interaction, complex formation, cytotoxicity, drug formulation, drug solubility, drug structure, fibroblast culture, in vitro study, isotherm, morphology, physical chemistry, schistosomiasis, spectroscopy
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Latin American Journal of Pharmacy, v. 29, n. 7, p. 1067-1074, 2010.