Prolonged retention of luliconazole nanofibers for topical mycotic condition: development, in vitro characterization and antifungal activity against Candida albicans

Abstract

An antifungal agent, luliconazole, is commercially available in cream or gel form. The major limitation of these conventional formulations is less residence time at the infection site. The primary objective of this work was to develop luliconazole-loaded polyvinyl alcohol (Luz-PVA) nanofibers for mycotic skin conditions with a longer retention. Luz-PVA nanofibers were prepared by plate electrospinning and optimized for polymer concentration and process parameters. The optimized batch (Trial 5) was prepared by 10% PVA, processed at 22.4 kV applied voltage, and 14 cm plate and spinneret distance to yield thick, uniform, and peelable nanofibers film. There was no interaction observed between Luz and PVA in the FTIR study. DSC and XRD analysis showed that luliconazole was loaded into fabricated nanofibers with a reduced crystallinity. FESEM studies confirmed the smooth, defect-free mats of nanofibers. Luz-PVA nanofibers possessed a tensile strength of 21.8 N and a maximum elongation of 10.8%, representing the excellent elasticity of the scaffolds. For Luz-PVA nanofibers, the sustained and complete drug release was observed in 48 h. In antifungal activity using Candida albicans, the Luz-PVA nanofibers showed a greater zone of inhibition (30.55 ± 0.38 mm and 29.27 ± 0.31 mm) than marketed cream (28.06 ± 0.18 mm and 28.47 ± 0.24 mm) and pure drug (27.57 ± 0.17 mm and 27.50 ± 0.47 mm) at 1% concentration in Sabouraud dextrose agar and yeast malt agar, respectively. Therefore, Luz-PVA nanofibers exhibited good mechanical properties, longer retention time, and better antifungal activity than marketed products and, therefore, can be further examined preclinically as a potential treatment option for topical mycotic infection.

Graphical Abstract