Novel transferosome formulation of Vemurafenib for skin cancer management: biocompatible and scalable strategies

Abstract Due to challenges such as poor aqueous solubility and compromised oral bioavailability, delivering Vemurafenib via a topical route using a scalable and biocompatible carrier-based hydrogel. This study aims to develop and characterize Vemurafenib-loaded transferosomes for the management of skin cancer. A Vemurafenib-loaded transferosomal gel was developed and thoroughly analyzed using various techniques, including transmission electron microscopy, ultraviolet spectroscopy, dermatokinetic parameters, entrapment efficiency, stability assessment, in vitro release study, vesicle elasticity examination, and antioxidant assays. The in vitro release of formulations was analyzed using four models: Korsmeyer, Higuchi, first-order, and zero-order models. The transferosomes exhibited a typical size of 105 nm, with a zeta size of 106.31 nm and a polydispersity index of 0.2417. Among the models investigated for in vitro release analysis, the Higuchi model was found to be the most suitable for the transferosome formulation. Compared to the standard formulation, the Vemurafenib-loaded transferosomal gel achieved a significantly higher concentration of 140.45 µg/ml on the skin epidermis within just 1.5 h. Additionally, in two hours, the Vemurafenib-loaded transferosomal gel resulted in a greater concentration of 118.52 µg/ml in the skin dermis, surpassing the usual formulation. Furthermore, the group receiving twice-daily administration of Vemurafenib-loaded transferosomal gel exhibited minimal hyperkeratosis compared to other treatment groups. The (3-(4, 5-dimethylthiazolyl-2)-2, 5-diphenyltetrazolium bromide) (MTT) assay showed a higher A-431 cell lines inhibition under vemurafenib Hydrogel formulation, i.e., 78.28%. This study offers compelling evidence for the effectiveness of the Vemurafenib transferosomal gel, demonstrating its enhanced skin absorption. The formulation shows considerable promise for further research and potential clinical application in skin cancer treatment.