Abstract
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.
Highlights
Nowadays, within the group of the most commonly encountered forms of infection, mycoses are the fourth ranked and, among them, superficial and skin fungal infections are the most frequent and widespread forms [1,2]
The results of this study demonstrated that the surfactants sucrose laurate and sucrose palmitate, in the presence of isopropyl alcohol as cosurfactant, are able to stabilize L/H microemulsion systems containing a mixture of essential oils and isopropyl myristate as the oil phase and water [56]
The microemulsions were prepared at room temperature, as described, by first mixing the oil phase with the surfactant–cosurfactant (SE-Isopropyl alcohol (IPA)) solution, FZ was dissolved into the respective mixture under moderated magnetic stirring (Hei-Tec hotplate magnetic stirrer, Heidolph, Schwabach, Germany)
Summary
Within the group of the most commonly encountered forms of infection, mycoses are the fourth ranked and, among them, superficial and skin fungal infections are the most frequent and widespread forms [1,2]. In oral therapy of skin mycoses, it was demonstrated that, compared with other azoles (itraconazole and ketoconazole) used in oral therapy of skin mycoses, FZ shows much higher affinity to the skin keratin and, it accumulates rapidly and greatly in the stratum corneum as an active, nonbinding form after systemic administration. This pharmacokinetic property of FZ largely accounts for its in vivo efficacy [8]. In the last two decades, the extensive investigations to improve FZ skin permeation were focused mainly on two directions: (1) the use of various chemical penetration enhancers incorporated in conventional topical dosage forms (emulsions, hydrogels, oleogels, emulgels and creams) [11–17]; and (2) the formulation of different nanocarrier systems such as vesicular nanocarriers (liposomes, ethosomes, oleic acid vesicles, nanostructure lipid carriers) and microemulsions, usually loaded in gel vehicles [18–25]
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