New, Biocompatible, Chitosan-Gelled Microemulsions Based on Essential Oils and Sucrose Esters as Nanocarriers for Topical Delivery of Fluconazole
Lavinia Vlaia,
Ioana Olariu,
Ana Maria Muţ,
Georgeta Coneac,
Vicenţiu Vlaia,
Dan Florin Anghel,
Monica Elisabeta Maxim,
Gabriela Stângă,
Amadeus Dobrescu,
Maria Suciu,
Zoltan Szabadai,
Dumitru Lupuleasa
Affiliations
Lavinia Vlaia
Department II—Pharmaceutical Technology, Formulation and Technology of Drugs Research Center, “Victor Babeș” University of Medicine and Pharmacy, 300041 Timișoara, Romania
Ioana Olariu
Department II—Pharmaceutical Technology, Formulation and Technology of Drugs Research Center, “Victor Babeș” University of Medicine and Pharmacy, 300041 Timișoara, Romania
Ana Maria Muţ
Department II—Pharmaceutical Technology, Formulation and Technology of Drugs Research Center, “Victor Babeș” University of Medicine and Pharmacy, 300041 Timișoara, Romania
Georgeta Coneac
Department II—Pharmaceutical Technology, Formulation and Technology of Drugs Research Center, “Victor Babeș” University of Medicine and Pharmacy, 300041 Timișoara, Romania
Vicenţiu Vlaia
Department I—Organic Chemistry, Formulation and Technology of Drugs Research Center, “Victor Babeș” University of Medicine and Pharmacy, 300041 Timișoara, Romania
Dan Florin Anghel
“Ilie Murgulescu” Institute of Physical Chemistry of the Romanian Academy, Laboratory of Colloid Chemistry, 060021 Bucharest, Romania
Monica Elisabeta Maxim
“Ilie Murgulescu” Institute of Physical Chemistry of the Romanian Academy, Laboratory of Colloid Chemistry, 060021 Bucharest, Romania
Gabriela Stângă
“Ilie Murgulescu” Institute of Physical Chemistry of the Romanian Academy, Laboratory of Colloid Chemistry, 060021 Bucharest, Romania
Amadeus Dobrescu
Department X Surgery 2–Surgery 2, “Victor Babeș” University of Medicine and Pharmacy, 300041 Timișoara, Romania
Maria Suciu
Department II—Pharmacology and Pharmacotherapy, “Victor Babeș” University of Medicine and Pharmacy, 300041 Timișoara, Romania
Zoltan Szabadai
National Institute for Research and Development in Electrochemistry and Condensed Matter, 300569 Timişoara, Romania
Dumitru Lupuleasa
Department of Pharmaceutical Technology and Biopharmaceutics, Faculty of Pharmacy, “Carol Davila” University of Medicine and Pharmacy, 020956 Bucharest, Romania
Biocompatible gel microemulsions containing natural origin excipients are promising nanocarrier systems for the safe and effective topical application of hydrophobic drugs, including antifungals. Recently, to improve fluconazole skin permeation, tolerability and therapeutic efficacy, we developed topical biocompatible microemulsions based on cinnamon, oregano or clove essential oil (CIN, ORG or CLV) as the oil phase and sucrose laurate (D1216) or sucrose palmitate (D1616) as surfactants, excipients also possessing intrinsic antifungal activity. To follow up this research, this study aimed to improve the adhesiveness of respective fluconazole microemulsions using chitosan (a biopolymer with intrinsic antifungal activity) as gellator and to evaluate the formulation variables’ effect (composition and concentration of essential oil, sucrose ester structure) on the gel microemulsions’ (MEGELs) properties. All MEGELs were evaluated for drug content, pH, rheological behavior, viscosity, spreadability, in vitro drug release and skin permeation and antifungal activity. The results showed that formulation variables determined distinctive changes in the MEGELs’ properties, which were nevertheless in accordance with official requirements for semisolid preparations. The highest flux and release rate values and large diameters of the fungal growth inhibition zone were produced by formulations MEGEL-FZ-D1616-CIN 10%, MEGEL-FZ-D1216-CIN 10% and MEGEL-FZ-D1616-ORG 10%. In conclusion, these MEGELs were demonstrated to be effective platforms for fluconazole topical delivery.
