Improvement of the oral praziquantel anthelmintic effect by cyclodextrin complexation


Autoria(s): de Jesus, Marcelo Bispo; Alves Pinto, Luciana de Matos; Fraceto, Leonardo Fernandes; Magalhaes, Luiz Augusto; Zanotti-Magalhaes, Eliana Maria; de Paula, Eneida
Contribuinte(s)

Universidade Estadual Paulista (UNESP)

Data(s)

20/05/2014

25/10/2016

20/05/2014

25/10/2016

01/01/2010

Resumo

Schistosomiasis is a parasitic disease which kills a half million people per year, a I I over the world. Praziquantel (PZQ) is the drug-of-choice for schistosomiasis because of its effectiveness, ease of administration, and low cost. However, poor solubility restricts its delivery, especially via the oral route. In this study, we describe beta-cyclodextrin (beta-CD) complexation as an alternative to improve the PZQ bioavailability. Physicochemical analysis were performed to characterize the inclusion complex formed between PZQ and beta-CD. Differential scanning calorimetry (DSC) thermograms and morphological analysis using scanning electronic microscopy (SEM) gave evidences of the complex formation. Diffusion NMR experiments allowed determination of the fraction of PZQ bound to beta-CD (37%) and the association constant (941 +/- 47 M(-1)). The in vivo evaluation of the complexation on the effect of PZQ was performed on mice infected with Schistosoma mansoni (BH strain); after 15 days of treatment with the PZQ:beta-CD complex the efficacy, evaluated by the number of remaining alive worms, was 99%, against 59% elicited by plain PZQ.

Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)

Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)

Identificador

Journal of Drug Targeting. Abingdon: Taylor & Francis Ltd, v. 18, n. 1, p. 21-26, 2010.

1061-186X

http://hdl.handle.net/11449/183

http://acervodigital.unesp.br/handle/11449/183

10.3109/10611860903131677

WOS:000274222800003

http://dx.doi.org/10.3109/10611860903131677

Idioma(s)

eng

Publicador

Taylor & Francis Ltd

Relação

Journal of Drug Targeting

Direitos

info:eu-repo/semantics/closedAccess

Palavras-Chave #Praziquantel #cyclodextrin #inclusion complex #schistosomiasis
Tipo

outro