Author(s):
Ruz Sanjuan, Vivian [UNESP] ; Van den Mooter, Guy ; Carlos, Iracilda Zeppone [UNESP] ; dos Santos Ramos, Matheus Aparecido [UNESP] ; Bauab, Taís Maria [UNESP] ; Tercini, Antonio Carlos Bergamaschi [UNESP] ; González Bedia, Mirtha Mayra ; Gomes de Oliveira, Anselmo [UNESP]
Date: 2020
Persistent ID: http://hdl.handle.net/11449/200382
Origin: Oasisbr
Subject(s): 2-(2-nitrovinyl) furan; Candida spp; Cyclodextrins inclusion complexes; Drug stabilization; Head space- gas chromatography; 2-(2-nitrovinyl) furan; 2-(2-nitrovinyl) furan; Candida spp; Candida spp; Cyclodextrins inclusion complexes; Cyclodextrins inclusion complexes; Drug stabilization; Drug stabilization; Head space- gas chromatography; Head space- gas chromatography
Description
Made available in DSpace on 2020-12-12T02:05:08Z (GMT). No. of bitstreams: 0 Previous issue date: 2020-08-01
Universidad Nacional de Salta
Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)
The 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.
São Paulo State University (UNESP) School of Pharmaceutical Sciences, Rodovia Araraquara-Jau, km 01
Drug Delivery and Disposition Department of Pharmaceutical and Pharmacological Sciences University of Leuven (KULeuven), O&N2 Herestraat 49-Box 921
São Paulo State University (UNESP) Center for Monitoring and Research Quality of Fuels Biofuels Petroleum and Derivatives (CEMPEQC) Chemistry Institute, Rua Prof. Francisco Degni 55
Pharmacy Department Chemistry and Pharmacy Faculty Central University of Las Villas, Carretera a Camajuaní km 5 ½
São Paulo State University (UNESP) School of Pharmaceutical Sciences, Rodovia Araraquara-Jau, km 01
São Paulo State University (UNESP) Center for Monitoring and Research Quality of Fuels Biofuels Petroleum and Derivatives (CEMPEQC) Chemistry Institute, Rua Prof. Francisco Degni 55
CAPES: 001
