Stability, biological and biopharmaceutical evaluation of the inclusion complexes of the antifungal and antiprotozoal drug candidate 2-(2-nitrovinyl) furan (G-0) with beta cyclodextrin derivatives

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Autor(es): dc.contributorUniversidade Estadual Paulista (Unesp)-
Autor(es): dc.contributorUniversity of Leuven (KULeuven)-
Autor(es): dc.contributorCentral University of Las Villas-
Autor(es): dc.creatorRuz Sanjuan, Vivian [UNESP]-
Autor(es): dc.creatorVan den Mooter, Guy-
Autor(es): dc.creatorCarlos, Iracilda Zeppone [UNESP]-
Autor(es): dc.creatordos Santos Ramos, Matheus Aparecido [UNESP]-
Autor(es): dc.creatorBauab, Taís Maria [UNESP]-
Autor(es): dc.creatorTercini, Antonio Carlos Bergamaschi [UNESP]-
Autor(es): dc.creatorGonzález Bedia, Mirtha Mayra-
Autor(es): dc.creatorGomes de Oliveira, Anselmo [UNESP]-
Data de aceite: dc.date.accessioned2022-02-22T00:30:26Z-
Data de disponibilização: dc.date.available2022-02-22T00:30:26Z-
Data de envio: dc.date.issued2020-12-11-
Data de envio: dc.date.issued2020-12-11-
Data de envio: dc.date.issued2020-08-01-
Fonte completa do material: dc.identifierhttp://dx.doi.org/10.1016/j.jddst.2020.101767-
Fonte completa do material: dc.identifierhttp://hdl.handle.net/11449/200382-
Fonte: dc.identifier.urihttp://educapes.capes.gov.br/handle/11449/200382-
Descrição: dc.descriptionThe purpose of this work was to evaluate the inclusion complexes (ICs) of 2-(2-nitrovinyl) furan (G-0) with hydroxypropyl and sulfobutylether-β-cyclodextrin intended for drug stabilization. The freeze-dried ICs were subjected to an accelerated stability study, monitored by HPLC-DAD and GC-MS methods. Drug sublimation/volatility has been analyzed through Thermogravimetric Analysis and Headspace Gas Chromatography. Drug dissolution profile in Simulated Vaginal Fluid (SVF) and permeation/retention in bovine vaginal mucosa were also evaluated. The influence of ICs on the “in vitro” antifungal activity against Candida spp. was investigated through Broth Microdilution Method and the cytotoxicity on fibroblasts and keratinocytes, through MTT assay protocol. ICs ensured an optimum drug chemical stability under accelerated conditions and significantly decreased the drug sublimation/volatilization compared with free G-0 and physical mixtures. Both complexes allowed a fast drug release in SVF, but G-0 was not quantified in the receptor compartment, although it was recovery from the mucosa, without significant influence on the complex formation. ICs maintained the antifungal activity against Candida albicans but improved the drug activity against a Candida krusei resistant strain (ICs MIC = 12.5 μg mL−1, G-0 MIC = 25 μg mL−1, Amphotericin B MIC = 20 μg mL−1). Cytotoxicity on fibroblast and keratinocytes followed the ranking order: G-0 > FD G-0/HP-β-CD > FD G-0/SBE-β-CD.-
Descrição: dc.descriptionUniversidad Nacional de Salta-
Descrição: dc.descriptionCoordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)-
Descrição: dc.descriptionSão Paulo State University (UNESP) School of Pharmaceutical Sciences, Rodovia Araraquara-Jau, km 01-
Descrição: dc.descriptionDrug Delivery and Disposition Department of Pharmaceutical and Pharmacological Sciences University of Leuven (KULeuven), O&N2 Herestraat 49-Box 921-
Descrição: dc.descriptionSão Paulo State University (UNESP) Center for Monitoring and Research Quality of Fuels Biofuels Petroleum and Derivatives (CEMPEQC) Chemistry Institute, Rua Prof. Francisco Degni 55-
Descrição: dc.descriptionPharmacy Department Chemistry and Pharmacy Faculty Central University of Las Villas, Carretera a Camajuaní km 5 ½-
Descrição: dc.descriptionSão Paulo State University (UNESP) School of Pharmaceutical Sciences, Rodovia Araraquara-Jau, km 01-
Descrição: dc.descriptionSão Paulo State University (UNESP) Center for Monitoring and Research Quality of Fuels Biofuels Petroleum and Derivatives (CEMPEQC) Chemistry Institute, Rua Prof. Francisco Degni 55-
Descrição: dc.descriptionCAPES: 001-
Idioma: dc.languageen-
Relação: dc.relationJournal of Drug Delivery Science and Technology-
???dc.source???: dc.sourceScopus-
Palavras-chave: dc.subject2-(2-nitrovinyl) furan-
Palavras-chave: dc.subjectCandida spp-
Palavras-chave: dc.subjectCyclodextrins inclusion complexes-
Palavras-chave: dc.subjectDrug stabilization-
Palavras-chave: dc.subjectHead space- gas chromatography-
Título: dc.titleStability, biological and biopharmaceutical evaluation of the inclusion complexes of the antifungal and antiprotozoal drug candidate 2-(2-nitrovinyl) furan (G-0) with beta cyclodextrin derivatives-
Tipo de arquivo: dc.typelivro digital-
Aparece nas coleções:Repositório Institucional - Unesp

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