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. 2022 May 4;27(9):2936.
doi: 10.3390/molecules27092936.

Novasomes as Nano-Vesicular Carriers to Enhance Topical Delivery of Fluconazole: A New Approach to Treat Fungal Infections

Iman Fatima  1 , Akhtar Rasul  1 , Shahid Shah  2 , Malik Saadullah  3 , Nayyer Islam  1 , Ahmed Khames  4 , Ahmad Salawi  5 , Muhammad Masood Ahmed  6 , Yosif Almoshari  5 , Ghulam Abbas  1 , Mohammed A S Abourehab  7   8 , Sajid Mehmood Khan  9 , Zunera Chauhdary  10 , Meshal Alshamrani  5 , Nader Ibrahim Namazi  11 , Demiana M Naguib  12
Affiliations

Novasomes as Nano-Vesicular Carriers to Enhance Topical Delivery of Fluconazole: A New Approach to Treat Fungal Infections

Iman Fatima et al. Molecules. .

Abstract

The occurrence of fungal infections has increased over the past two decades. It is observed that superficial fungal infections are treated by conventional dosage forms, which are incapable of treating deep infections due to the barrier activity possessed by the stratum corneum of the skin. This is why the need for a topical preparation with advanced penetration techniques has arisen. This research aimed to encapsulate fluconazole (FLZ) in a novasome in order to improve the topical delivery. The novasomes were prepared using the ethanol injection technique and characterized for percent entrapment efficiency (EE), particle size (PS), zeta potential (ZP), drug release, Fourier-transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), thermogravimetric analysis (TGA), scanning electron microscopy (SEM) and antifungal activity. The FN7 formulation with 94.45% EE, 110 nm PS and -24 ZP proved to be the best formulation. The FN7 formulation showed a 96% release of FLZ in 8 h. FTIR showed the compatibility of FLZ with excipients and DSC studies confirmed the thermal stability of FLZ in the developed formulation. The FN7 formulation showed superior inhibition of the growth of Candida albicans compared to the FLZ suspension using a resazurin reduction assay, suggesting high efficacy in inhibiting fungal growth.

Keywords: antifungal activity; ethanol injection technique; fluconazole; novasomes; toxicity study.

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Conflict of interest statement

The authors declare no conflict of interest.

Figures

Figure 1
Figure 1
PS (A) and ZP (B) of optimum formulation FN7 showed a particle size of 110 nm and a ZP value of −24.
Figure 2
Figure 2
The release of FLZ from prepared novasomes containing different ratios of FFAs and SAAs.
Figure 3
Figure 3
FTIR spectra of cholesterol (A), oleic acid (B), Span 60 (C), FLZ (D), drug-unloaded FN7 (E) and FLZ-loaded FN7 (F).
Figure 4
Figure 4
DSC thermograms (A) and TGA (B) of FLZ (A), oleic acid (B), Span 60 (C), cholesterol (D), blank formulation (E) and FLZ-loaded formulation (F).
Figure 5
Figure 5
SEM images of drug-unloaded (A–C) and FLZ-loaded (D–F) formulations at different resolutions.
Figure 6
Figure 6
Percentage (%) of inhibition (A–C) and zone of inhibition (D). Values are expressed as mean ± SEM (n = 5), ns = non-significant compared to FLZ suspension. Antifungal activity of FN7, unloaded novasomes, FLZ suspension and standard drug (E).
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