Journal of Drug Delivery Science and Technology, 2020
Abstract The purpose of this work was to evaluate the inclusion complexes (ICs) of 2-(2-nitroviny... more Abstract 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.
Context: Full factorial design is effective in predicting the properties optimization and process... more Context: Full factorial design is effective in predicting the properties optimization and processing conditions of cosmetic emulsions. However, in most factorial designs, the technological quality and accelerated stability tests of emulsions are not included together as dependent variables. Aims: To predict the technological quality and physical stability of model cosmetic emulsions from the combination of formulation and processing factors using a 23 full factorial design. Methods: A 23 full factorial design with 95 % of confidence was generated in order to evaluate the influence of critical factors during the manufacture of cosmetic emulsions on their quality and physical stability. Emulsifier, concentration of stearic acid (formulation factors) and type of cooling (processing factor) were the independent variables, whereas spreadability, bulk density and pH were dependent variables for technological quality and centrifugation, heating-cooling and freeze-thaw cycles were dependent...
Journal of Drug Delivery Science and Technology, 2020
Abstract The purpose of this work was to evaluate the inclusion complexes (ICs) of 2-(2-nitroviny... more Abstract 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.
Context: Full factorial design is effective in predicting the properties optimization and process... more Context: Full factorial design is effective in predicting the properties optimization and processing conditions of cosmetic emulsions. However, in most factorial designs, the technological quality and accelerated stability tests of emulsions are not included together as dependent variables. Aims: To predict the technological quality and physical stability of model cosmetic emulsions from the combination of formulation and processing factors using a 23 full factorial design. Methods: A 23 full factorial design with 95 % of confidence was generated in order to evaluate the influence of critical factors during the manufacture of cosmetic emulsions on their quality and physical stability. Emulsifier, concentration of stearic acid (formulation factors) and type of cooling (processing factor) were the independent variables, whereas spreadability, bulk density and pH were dependent variables for technological quality and centrifugation, heating-cooling and freeze-thaw cycles were dependent...
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