Alternativas para o tratamento da esquistossomose: Caracterizacao fisico-quimica do complexo de inclusao entre praziquantel e hidroxipropil-β-ciclodextrina


Autoria(s): Chaves, Izabel S.; Rodrigues, Stella G.; Melo, Nathalie F.S.; de Jesus, Marcelo B.; Fraceto, Leonardo F.; de Paula, Eneida; Pinto, Luciana M.A.
Contribuinte(s)

Universidade Estadual Paulista (UNESP)

Data(s)

27/05/2014

27/05/2014

01/12/2010

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.

Formato

1067-1074

Identificador

http://www.latamjpharm.org/resumenes/29/7/LAJOP_29_7_1_2.pdf

Latin American Journal of Pharmacy, v. 29, n. 7, p. 1067-1074, 2010.

0326-2383

http://hdl.handle.net/11449/72173

2-s2.0-78650807875

Idioma(s)

por

Relação

Latin American Journal of Pharmacy

Direitos

closedAccess

Palavras-Chave #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
Tipo

info:eu-repo/semantics/article