5-Fluorouracil- and Sesamol-Loaded Transliposomal Gel for Skin Cancer: <i>In Vitro, Ex Vivo</i>, and Dermatokinetic Evaluation
Samreen Jahan, Niha Sultana, Asad Ali, Asad Ali, Nasr A. Emad, Perwez Alam, Mohd Mujeeb, Mohd. Aqil, Asgar Ali, Asgar Ali
Abstract
High Resolution Image Download MS PowerPoint Slide This study explores a novel approach to managing skin conditions through a combination therapy utilizing a phospholipid-enriched edge activator-based nanoformulation. 5-Fluorouracil (5-FU)- and sesamol (SES)-loaded transliposomes (FS-TL) were developed using a thin film hydration method and optimized using Box-Behnken Design. FS-TL characterization indicated a vesicle size of 165.6 ± 1.1 nm, polydispersity index of 0.28 ± 0.01, and a zeta potential of −33.17 ± 0.9 mV, and the percent entrapment efficiencies for 5-FU and SES were found to be 63.16 ± 1.07% and 75.60 ± 3.68%, respectively. The drug loading percents for 5-FU and SES were found to be 5.87 ± 0.099% and 7.03 ± 0.34%, respectively. The morphological studies exhibit the distinctive spherical shape of the nanoformulation. The in vitro drug release demonstrated sustained release with 82.52 ± 1.2% and 86.28 ± 1.3% releases for 5-FU and SES, respectively. The ex vivo skin permeation exhibited 81.04 ± 2.1% and 78.03 ± 1.7% for 5-FU and SES. Confocal laser microscopy scanning (CLSM) revealed a deeper formulation penetration (30.0 μm) of excised mice skin membranes than for a standard rhodamine solution (10.0 μm). The dermatokinetic investigation revealed that FS-TL gel has significantly higher concentrations of 5-FU and SES ( p < 0.001). The efficacy of FS-TL ( p < 0.05) in eradicating the A431 melanoma cell line was satisfactory. These findings suggest the potential of FS-TL formulation over conventional approaches in skin cancer management.