Improved Topical Antifungal Medication using Sertaconazole Bilosomes: In vitro Permeability, Cytotoxicity, and Clinical Assessment

Objective: The purpose of the current study was to develop Sertaconazole bilosomes (SBs) with enhanced permeability, skin deposition, anti-fungal properties, and clinical efficacy. Methods: By changing span 60 to cholesterol molar ratio, bile salt type, and concentration, 12 formulations of SBs were prepared using the thin film hydration method and characterized by particle size (PS), zeta potential (ZP), polydispersity index (PDI), % entrapment efficiency (% EE), and % cumulative drug released after 8h (% Q8h ) and 24h (% Q24h). The optimized formulation (SB 5) was incorporated into 1% Carbopol 940 hydrogel (SBG 5) and tested for ex-vivo permeability, skin deposition, and anti-fungal efficacy compared to the commercial formulation (Dermofix® cream) and sertaconazole alone hydrogel (SAG). A randomized controlled clinical trial of SBG 5 compared to Dermofix® cream and SAG was done on 30 patients diagnosed with Tinea corporis with a 4-week follow-up. Results: SB 5 showed PS of 158 ± 6.4nm, ZP of −55 ± 1.7mV, PDI of 0.16 ± 0.01, % EE of 96 ± 3.4, % Q8h of  70.3 ± 3.6, and % Q24h of  97.2 ± 3.0. SBG 5 exhibited in vitro release after 24h (1.25 and 1.51-fold), skin permeability (1.6 and 2.3-fold), skin deposition (3.86 and 14.82-fold), and anti-fungal efficacy against Candida albicans (two and 1.44-fold) compared to Dermofix® cream and SAG respectively. Patients receiving SBG 5 exhibited a 1.25 and 1.8-fold higher recovery rate on days 14 and 21 respectively compared to Dermofix® cream, and a 4.5 and two-fold recovery rate on days 14 and 21 respectively compared to SAG. Conclusion: Bilosomes could be utilized to enhance permeability, skin deposition, anti-fungal properties, and clinical efficacy of Sertaconazole.