Improvement of the oral praziquantel anthelmintic effect by cyclodextrin complexation

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dc.contributor.authorde Jesus, Marcelo Bispo
dc.contributor.authorAlves Pinto, Luciana de Matos
dc.contributor.authorFraceto, Leonardo Fernandes [UNESP]
dc.contributor.authorMagalhaes, Luiz Augusto
dc.contributor.authorZanotti-Magalhaes, Eliana Maria
dc.contributor.authorde Paula, Eneida
dc.contributor.institutionUniversidade Estadual de Campinas (UNICAMP)
dc.contributor.institutionUniversidade Federal de Lavras (UFLA)
dc.contributor.institutionUniversidade Estadual Paulista (Unesp)
dc.date.accessioned2014-05-20T13:12:12Z
dc.date.available2014-05-20T13:12:12Z
dc.date.issued2010-01-01
dc.description.abstractSchistosomiasis 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.en
dc.description.affiliationState Univ Campinas UNICAMP, Inst Biol, Dept Biochem, BR-13083970 Campinas, SP, Brazil
dc.description.affiliationUniversidade Federal de Lavras (UFLA), Dept Chem, Lavras, MG, Brazil
dc.description.affiliationSão Paulo State Univ, Dept Environm Engn, Sorocaba, SP, Brazil
dc.description.affiliationUniv Estadual Campinas, Dept Parasitol, Inst Biol, Campinas, SP, Brazil
dc.description.affiliationUnespSão Paulo State Univ, Dept Environm Engn, Sorocaba, SP, Brazil
dc.description.sponsorshipFundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)
dc.description.sponsorshipConselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)
dc.description.sponsorshipIdFAPESP: 06/03838-1
dc.description.sponsorshipIdFAPESP: 02/04103-4
dc.format.extent21-26
dc.identifierhttp://dx.doi.org/10.3109/10611860903131677
dc.identifier.citationJournal of Drug Targeting. Abingdon: Taylor & Francis Ltd, v. 18, n. 1, p. 21-26, 2010.
dc.identifier.doi10.3109/10611860903131677
dc.identifier.issn1061-186X
dc.identifier.urihttp://hdl.handle.net/11449/183
dc.identifier.wosWOS:000274222800003
dc.language.isoeng
dc.publisherTaylor & Francis Ltd
dc.relation.ispartofJournal of Drug Targeting
dc.relation.ispartofjcr3.408
dc.rights.accessRightsAcesso restrito
dc.sourceWeb of Science
dc.subjectPraziquantelen
dc.subjectcyclodextrinen
dc.subjectinclusion complexen
dc.subjectschistosomiasisen
dc.titleImprovement of the oral praziquantel anthelmintic effect by cyclodextrin complexationen
dc.typeArtigo
dcterms.licensehttp://informahealthcare.com/page/resources/authors
dcterms.rightsHolderTaylor & Francis Ltd
unesp.author.orcid0000-0002-2827-2038[3]
unesp.author.orcid0000-0003-0812-1491[1]
unesp.campusUniversidade Estadual Paulista (Unesp), Instituto de Ciência e Tecnologia, Sorocabapt

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Artigos - Engenharia Ambiental - Sorocaba