No abstract

Multilayer films from hydrophobically modified poly(acrylic acid) (HMPA) and their complexes with cationic surfactants were successfully prepared using the layer-by-layer (LbL) method. Alkyl trimethylammonium bromide derivatives with various lengths of the hydrophobic chain (C10–C18) were used to interact with the HMPA polymer, generating highly hydrophobic domains in the films and contributing to the antimicrobial properties of the prepared coating. The antimicrobial efficiency against common pathogens such as Staphylococcus aureus, Escherichia coli, Pseudomonas aeruginosa, and Candida albicans was investigated in relationship with the morphology and composition of the thin films. The wettability and roughness of the multilayered systems were evaluated using atomic force microscopy (AFM) and contact angle measurements. The effects of the microbial exposure on the surface properties of the prepared films were investigated in order to assess the stability of the HMPA-deposited multilayers and the durability of the antimicrobial activity. The hydrophobically modified films exhibited antimicrobial activity against the studied pathogens. The best efficiency was registered in the case of S. aureus, which showed an inhibition of growth up to 100% after 2 h. C. albicans proved to be less sensitive to the effect of the multilayers deposited from HMPA–surfactant complexes. These results suggest that HMPA and HMPA–surfactant complex LbL multilayer films can be used as promising materials in antimicrobial surface coatings with increased resistance to pathogens during exposure.

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.

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.

No abstract