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

• Published in: Molecules (Basel, Switzerland) Switzerland), 2022-05, Vol.27 (9), p.2936
• Main Authors: Fatima, Iman, Rasul, Akhtar, Shah, Shahid, Saadullah, Malik, Islam, Nayyer, Khames, Ahmed, Salawi, Ahmad, Ahmed, Muhammad Masood, Almoshari, Yosif, Abbas, Ghulam, Abourehab, Mohammed A S, Mehmood Khan, Sajid, Chauhdary, Zunera, Alshamrani, Meshal, Namazi, Nader Ibrahim, Naguib, Demiana M
• Format: Article
• Language: English
• Subjects: Antifungal activity; Antifungal agents; Antifungal Agents - therapeutic use; Calorimetry; Candida albicans; Cholesterol; Differential scanning calorimetry; Drug Carriers - chemistry; Drug delivery systems; Drug Delivery Systems - methods; Efficiency; Entrapment; Ethanol; ethanol injection technique; Fluconazole; Fluconazole - chemistry; Fluconazole - pharmacology; Fungal infections; Fungi; Fungicides; Infections; Infrared analysis; Infrared spectroscopy; Mycoses - drug therapy; novasomes; Particle Size; Scanning electron microscopy; Skin; Spectrum analysis; Stratum corneum; Thermal stability; Thermogravimetric analysis; toxicity study; Zeta potential
• ISSN: 1420-3049; 1420-3049
• DOI: 10.3390/molecules27092936

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 compared to the FLZ suspension using a resazurin reduction assay, suggesting high efficacy in inhibiting fungal growth.