article · Drug Delivery
Fenticonazole nitrate is an antifungal drug with poor water solubility, limiting its effectiveness when applied to the skin. To address this, the drug was encapsulated into trans-novasomes, which are specialised lipid nanovesicles containing edge activators alongside standard novasome components to improve topical delivery. Using an ethanol injection technique guided by experimental design, several formulations were produced and evaluated. The most effective formulation achieved complete drug entrapment, nanoscale droplet size, and stable surface charge. Computational simulations confirmed stable interactions between the drug and formulation lipids. In laboratory tests, this formulation showed superior inhibition of the fungus Trichophyton mentagrophytes compared to a standard drug suspension. Furthermore, an exploratory clinical study in patients with tinea corporis demonstrated that the formulation outperformed a commercially available antifungal cream in achieving clinical cures, presenting an enhanced topical formulation approach.
Fungal skin infections such as tinea corporis are common, but many antifungal drugs struggle to penetrate the skin effectively due to poor water solubility. Developing lipid nanoparticle carriers that enhance drug delivery directly to infected tissue can significantly improve patient recovery. Demonstrating higher cure rates than existing commercial treatments points to more reliable, fast-acting topical therapies for dermatological conditions.
This work provides an applied nanocarrier formulation for pharmaceutical manufacturers and dermatology clinicians seeking to improve topical antifungal therapies. Having progressed through laboratory characterisation, computational validation, and an initial comparative clinical assessment in human patients, the technology sits at an applied and clinically tested stage. Further scale-up and expanded clinical trials would be required before this formulation could be commercialised as a replacement or competitor to existing topical antifungal creams.
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The current investigation aimed for loading fenticonazole nitrate (FTN), an antifungal agent with low aqueous solubility, into trans-novasomes (TNs) for management of tinea corporis topically. TNs contain Brij<sup>®</sup> as an edge activator besides the components of novasomes (cholesterol, Span 60, and oleic acid) owing to augment the topical delivery of FTN. TNs were fabricated applying ethanol injection method based on D-optimal experiment. TNs were evaluated with regard to entrapment efficiency percent (EE%), particle size (PS), polydispersity index (PDI), and zeta potential (ZP). Further explorations were conducted on the optimum formulation (F7). F7 showed spherical appearance with EE%, PS, PDI, and ZP of 100.00 ± 1.10%, 358.60 ± 10.76 nm, 0.51 ± 0.004, and -30.00 ± 0.80 mV, respectively. The <i>in silico</i> study revealed the ability of the FTN-cholesterol complex to maintain favorable interactions throughout the molecular dynamics simulation (MDS) study. Moreover, <i>Trichophyton mentagrophytes</i> growth was inhibited effectively by F7 than by FTN suspension applying 2,3-bis(2-methyloxy-4-nitro-5-sulfophenyl)-2H-tetrazolium-5-carboxanilide (XTT) reduction assay. Furthermore, a clinical appraisal on patients with tinea corporis fungal lesions confirmed the superiority of F7 compared to Miconaz<sup>®</sup> cream in the magnitude of clinical cure of tinea corporis. Thereby, TNs could be considered as promising vesicles for enhancing the antifungal potential of FTN for the topical management of tinea corporis.
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DOI: 10.1080/10717544.2022.2057619
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