Development and physicochemical characterization of solid dispersions containing praziquantel for the treatment of schistosomiasis

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dc.contributor.authorDametto, P. R.
dc.contributor.authorDametto, A. C. [UNESP]
dc.contributor.authorPolese, L. [UNESP]
dc.contributor.authorRibeiro, C. A. [UNESP]
dc.contributor.authorChorilli, M. [UNESP]
dc.contributor.authorde Freitas, Osvaldo
dc.contributor.institutionUniversidade de São Paulo (USP)
dc.contributor.institutionUniversidade Estadual Paulista (Unesp)
dc.date.accessioned2018-12-11T17:29:15Z
dc.date.available2018-12-11T17:29:15Z
dc.date.issued2017-02-01
dc.description.abstractPraziquantel (PZQ) is an anthelminthic agent active against parasitic flatworms of the Schistosoma type and the most important drug for the treatment and morbidity control of schistosomiasis. In this study, a high-performance liquid chromatography method was employed for quantification of PZQ in the physical mix (PM) and solid dispersion (SD) prepared by Fusion Method utilizing the carriers Gelucire® 50/13 and mannitol in ratio 3:1; 1:1; 1:3 PZQ/carrier. Furthermore, PM and SD were characterized by Thermogravimetry–Differential Thermal Analysis, Differential Scanning Calorimetry, Infrared Spectroscopy, X-Ray Diffraction, and Scanning Electron Microscopy. Solubility assay was made to evaluate the solubility of PZQ in purified water, in 0.1 mol L−1 HCl solution and 0.2 mol L−1 buffered phosphate solution. PZQ dissolution test was carried out in 0.1 mol L−1 HCl and 0.2 M buffered phosphate (pH 6.8). The interaction between PZQ and carriers in PMs and SDs was evidenced due to experimental enthalpy, which was different from expected enthalpy. However, this interaction did not affect the solubility of the drug. In PZQ dissolution test, the best result was for SD 1:1 PZQ/Gelucire, which presented higher dissolution rate and release extension than PM and PZQ. Thus, SD may be a strategy to enhance the solubility and dissolution, a crucial step in the development of a pharmaceutical dosage form containing PZQ for possible application in the treatment of schistosomiasis.en
dc.description.affiliationFaculdade de Ciências Farmacêuticas USP
dc.description.affiliationInstituto de Química UNESP
dc.description.affiliationInstituto de Biociências UNESP
dc.description.affiliationFaculdade de Ciências Farmacêuticas UNESP
dc.description.affiliationUnespInstituto de Química UNESP
dc.description.affiliationUnespInstituto de Biociências UNESP
dc.description.affiliationUnespFaculdade de Ciências Farmacêuticas UNESP
dc.description.sponsorshipFundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)
dc.description.sponsorshipIdFAPESP: 2011/11586-0
dc.format.extent1693-1706
dc.identifierhttp://dx.doi.org/10.1007/s10973-016-5759-1
dc.identifier.citationJournal of Thermal Analysis and Calorimetry, v. 127, n. 2, p. 1693-1706, 2017.
dc.identifier.doi10.1007/s10973-016-5759-1
dc.identifier.file2-s2.0-84982182090.pdf
dc.identifier.issn1588-2926
dc.identifier.issn1388-6150
dc.identifier.lattes8498310891810082
dc.identifier.orcid0000-0002-7984-5908
dc.identifier.scopus2-s2.0-84982182090
dc.identifier.urihttp://hdl.handle.net/11449/178200
dc.language.isoeng
dc.relation.ispartofJournal of Thermal Analysis and Calorimetry
dc.relation.ispartofsjr0,587
dc.relation.ispartofsjr0,587
dc.rights.accessRightsAcesso aberto
dc.sourceScopus
dc.subjectHPLC–UV
dc.subjectPhysical mix
dc.subjectPraziquantel
dc.subjectSolid dispersion
dc.titleDevelopment and physicochemical characterization of solid dispersions containing praziquantel for the treatment of schistosomiasisen
dc.typeArtigo
unesp.author.lattes8498310891810082[4]
unesp.author.orcid0000-0002-7984-5908[4]
unesp.departmentFármacos e Medicamentos - FCFpt

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