Advancements in skin cancer treatment: 5-fluorouracil and carvedilol-loaded transethosomes using Lipoid S100.

Objective: This study investigates a hybrid drug delivery system combination of 5-Fluorouracil (5-FU) and Carvedilol (CVD) for enhanced chemotherapeutic efficacy in skin cancer treatment. The approach addresses challenges such as drug resistance and suboptimal delivery in conventional therapies.

Methods: Transethosomes (TEs) were developed using the Modified Ethanol Injection method, with optimization based on the concentrations of Lipoid S100, Tween 80, Polyvinyl Alcohol, and ethanol via the Box-Behnken Design. Characterization techniques, including FT-IR, DSC, Raman spectroscopy, XRD, FESEM, TEM, and AFM, were utilized to evaluate the formulations. In vitro anticancer studies, including IC50 determination, MTT assays, and cell cycle analysis, were conducted alongside drug permeation and hemolysis evaluations performed in vitro and ex vivo.

Results: The optimized transethosome formulation demonstrated a particle size of 113 nm, a zeta potential of 27.23 mV, and encapsulation efficiencies of 97.21% for 5-FU and 98.73% for CVD. Spectroscopic analyses indicated no significant drug-excipient interactions, while XRD confirmed the amorphous nature of the drug in the formulation. Microscopy revealed spherical vesicles with uniform coating. The formulation showed significant anticancer activity in in vitro studies.

Conclusion: The combination of 5-FU and CVD within a transethosome-based delivery system presents a potential alternative for topical chemotherapy in skin cancer treatment, offering enhanced therapeutic efficacy. This study underscores the potential of hybrid drug carriers in advancing targeted cancer therapies.