Transdermal delivery of lornoxicam via transethosomal gel as a novel strategy for management of rheumatoid arthritis.

OBJECTIVE

This study aimed to develop and optimize lornoxicam-loaded transethosomal vesicles (LOR-TES) to improve the solubility, skin permeation, and transdermal delivery of lornoxicam for potential use in the treatment of rheumatoid arthritis.

METHODS

LOR-TES formulations were prepared using the thin-film hydration method. A Box-Behnken design (BBD) was employed to evaluate the influence of formulation variables, such as lipid content, ethanol concentration, and surfactant amount. The optimized vesicles were incorporated into a Carbopol-based gel using the soaking method and refined through a hit-and-trial approach. The formulations were characterized for particle size (PS), polydispersity index (PDI), zeta potential (ZP), and entrapment efficiency (%EE). Surface morphology was assessed using scanning electron microscopy (SEM), while compatibility and encapsulation were confirmed via Fourier-transform infrared spectroscopy (FTIR) and differential scanning calorimetry (DSC). In vitro drug release, ex vivo skin permeation using Franz diffusion cells, and stability studies over six months were conducted.

RESULTS

The optimized LOR-TES showed a PS of 150.7 ± 1.2 nm, PDI of 0.326 ± 0.04, a ZP of -23.3 ± 0.9 mV, and %EE of 80.9 ± 0.2%. SEM revealed spherical morphology, while FTIR and DSC confirmed compatibility and successful encapsulation. In vitro release studies showed sustained drug release, and ex vivo studies demonstrated a fourfold increase in skin permeation from the LOR-TES gel compared to the conventional formulation. Stability testing confirmed formulation stability.

CONCLUSIONS

The developed LOR-TES gel enhanced transdermal drug delivery, offering sustained release and improved permeation. It presents a promising strategy for effective management of rheumatoid arthritis through the transdermal route.