1. Topical Biocompatible Fluconazole-Loaded Microemulsions Based on Essential Oils and Sucrose Esters: Formulation Design Based on Pseudo-Ternary Phase Diagrams and Physicochemical Characterization
- Author
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Vicenţiu Vlaia, Georgeta Coneac, Mircea Hîrjău, Amadeus Dobrescu, Monica Elisabeta Maxim, Lavinia Vlaia, Ioana Olariu, Dan F. Anghel, Dumitru Lupuleasa, and Ana Maria Muţ
- Subjects
pseudo-ternary phase diagram ,Dispersity ,Bioengineering ,02 engineering and technology ,lcsh:Chemical technology ,030226 pharmacology & pharmacy ,essential oil ,law.invention ,biocompatible sucrose ester ,lcsh:Chemistry ,03 medical and health sciences ,Viscosity ,chemistry.chemical_compound ,0302 clinical medicine ,law ,Stearate ,Phase (matter) ,fluconazole ,Zeta potential ,Chemical Engineering (miscellaneous) ,Microemulsion ,lcsh:TP1-1185 ,Solubility ,Essential oil ,Chromatography ,Chemistry ,Process Chemistry and Technology ,021001 nanoscience & nanotechnology ,microemulsion ,lcsh:QD1-999 ,0210 nano-technology - Abstract
To initiate our research into the development of biocompatiî, le gelled-microemulsions based on essential oils (EOs) and sucrose esters (SEs) for the topical delivery of fluconazole, this formulation study investigated the usefulness of two relatively harmless natural non-ionic surfactants from the group of SEs (sucrose laurate and stearate) to form, in the presence of antifungal EOs, stable, isotropic microemulsions effective on fluconazole solubilization. Fluconazole&rsquo, s solubility in EO significantly depended on their chemical composition, showing higher values for cinnamon, oregano and clove essential oils, further selected as oil phase components for microemulsion formulations. The phase behavior of several EO&ndash, isopropyl miristate/SE&ndash, isopropanol/water systems was assessed through pseudo-ternary phase diagrams constructed by microplate dilution technique. The hydrocarbon chain length of the SE and EO type strongly influenced the size of the microemulsion region in the pseudo-ternary phase diagrams. Ten microemulsion formulations containing 2% fluconazole, 6% or 10% oil mixture of EO&ndash, isopropyl myristate in 1:1 ratio, 45% SE-isopropanol mixture and water, were selected and evaluated for physicochemical properties (droplet size, polydispersity, viscosity, refractive index, zeta potential and pH). All formulations were physicochemically acceptable, but viscosity enhancement and further in vitro and in vivo tests are required for the development of biocompatible, clinically safe and effective fluconazole topical preparations.
- Published
- 2021