LAPSE:2023.24962
Published Article
LAPSE:2023.24962
Topical Biocompatible Fluconazole-Loaded Microemulsions Based on Essential Oils and Sucrose Esters: Formulation Design Based on Pseudo-Ternary Phase Diagrams and Physicochemical Characterization
March 28, 2023
Abstract
To initiate our research into the development of biocompatiîle 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’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−isopropyl miristate/SE−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−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.
To initiate our research into the development of biocompatiîle 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’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−isopropyl miristate/SE−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−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.
Record ID
Keywords
biocompatible sucrose ester, essential oil, fluconazole, microemulsion, pseudo-ternary phase diagram
Subject
Suggested Citation
Vlaia L, Coneac G, Muţ AM, Olariu I, Vlaia V, Anghel DF, Maxim ME, Dobrescu A, Hîrjău M, Lupuleasa D. Topical Biocompatible Fluconazole-Loaded Microemulsions Based on Essential Oils and Sucrose Esters: Formulation Design Based on Pseudo-Ternary Phase Diagrams and Physicochemical Characterization. (2023). LAPSE:2023.24962
Author Affiliations
Vlaia L: Department II—Pharmaceutical Technology, Formulation and Technology of Drugs Research Center, “Victor Babeș” University of Medicine and Pharmacy, Eftimie Murgu Sq. no. 2, 300041 Timișoara, Romania
Coneac G: Department II—Pharmaceutical Technology, Formulation and Technology of Drugs Research Center, “Victor Babeș” University of Medicine and Pharmacy, Eftimie Murgu Sq. no. 2, 300041 Timișoara, Romania
Muţ AM: Department II—Pharmaceutical Technology, Formulation and Technology of Drugs Research Center, “Victor Babeș” University of Medicine and Pharmacy, Eftimie Murgu Sq. no. 2, 300041 Timișoara, Romania
Olariu I: Department II—Pharmaceutical Technology, Formulation and Technology of Drugs Research Center, “Victor Babeș” University of Medicine and Pharmacy, Eftimie Murgu Sq. no. 2, 300041 Timișoara, Romania
Vlaia V: Department I—Organic Chemistry, Formulation and Technology of Drugs Research Center, “Victor Babeș” University of Medicine and Pharmacy, Eftimie Murgu Sq. no. 2, 300041 Timișoara, Romania
Anghel DF: Laboratory of Colloid Chemistry, “Ilie Murgulescu” Institute of Physical Chemistry of the Romanian Academy, Splaiul Independenţei 202, 060021 Bucharest, Romania
Maxim ME: Laboratory of Colloid Chemistry, “Ilie Murgulescu” Institute of Physical Chemistry of the Romanian Academy, Splaiul Independenţei 202, 060021 Bucharest, Romania
Dobrescu A: Department X Surgery 2—Surgery 2, “Victor Babeș” University of Medicine and Pharmacy, Eftimie Murgu Sq. no. 2, 300041 Timișoara, Romania [ORCID]
Hîrjău M: Department of Pharmaceutical Technology and Biopharmaceutics, Faculty of Pharmacy, “Carol Davila” University of Medicine and Pharmacy, Traian Vuia no.6, 020956 Bucharest, Romania
Lupuleasa D: Department of Pharmaceutical Technology and Biopharmaceutics, Faculty of Pharmacy, “Carol Davila” University of Medicine and Pharmacy, Traian Vuia no.6, 020956 Bucharest, Romania
Coneac G: Department II—Pharmaceutical Technology, Formulation and Technology of Drugs Research Center, “Victor Babeș” University of Medicine and Pharmacy, Eftimie Murgu Sq. no. 2, 300041 Timișoara, Romania
Muţ AM: Department II—Pharmaceutical Technology, Formulation and Technology of Drugs Research Center, “Victor Babeș” University of Medicine and Pharmacy, Eftimie Murgu Sq. no. 2, 300041 Timișoara, Romania
Olariu I: Department II—Pharmaceutical Technology, Formulation and Technology of Drugs Research Center, “Victor Babeș” University of Medicine and Pharmacy, Eftimie Murgu Sq. no. 2, 300041 Timișoara, Romania
Vlaia V: Department I—Organic Chemistry, Formulation and Technology of Drugs Research Center, “Victor Babeș” University of Medicine and Pharmacy, Eftimie Murgu Sq. no. 2, 300041 Timișoara, Romania
Anghel DF: Laboratory of Colloid Chemistry, “Ilie Murgulescu” Institute of Physical Chemistry of the Romanian Academy, Splaiul Independenţei 202, 060021 Bucharest, Romania
Maxim ME: Laboratory of Colloid Chemistry, “Ilie Murgulescu” Institute of Physical Chemistry of the Romanian Academy, Splaiul Independenţei 202, 060021 Bucharest, Romania
Dobrescu A: Department X Surgery 2—Surgery 2, “Victor Babeș” University of Medicine and Pharmacy, Eftimie Murgu Sq. no. 2, 300041 Timișoara, Romania [ORCID]
Hîrjău M: Department of Pharmaceutical Technology and Biopharmaceutics, Faculty of Pharmacy, “Carol Davila” University of Medicine and Pharmacy, Traian Vuia no.6, 020956 Bucharest, Romania
Lupuleasa D: Department of Pharmaceutical Technology and Biopharmaceutics, Faculty of Pharmacy, “Carol Davila” University of Medicine and Pharmacy, Traian Vuia no.6, 020956 Bucharest, Romania
Journal Name
Processes
Volume
9
Issue
1
First Page
pr9010144
Year
2021
Publication Date
2021-01-13
ISSN
2227-9717
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PII: pr9010144, Publication Type: Journal Article
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LAPSE:2023.24962
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https://doi.org/10.3390/pr9010144
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