Transferosome-assisted transdermal delivery of rivaroxaban: formulation and evaluation

Rivaroxaban (RIV) is an orally active, selective, direct factor Xa inhibitor used for the prevention and treatment of venous thromboembolism, stroke prevention in non-valvular atrial fibrillation, and other thromboembolic disorders. This research developed RIV-loaded transferosomes as a non-invasive option for individuals who cannot administer oral anticoagulants. Twenty RIV transfersomal formulations (F1–F20) were prepared by the rotary evaporation–sonication method using lecithin and various edge activators (Soluplus, Span 65, Span 80, and Tween 20) at different phospholipid-to-edge activator ratios. RIV transfersomal formulations (F1–F20) were evaluated for drug content, entrapment efficiency, vesicle size, polydispersity index, and pH. The lead transfersomal RIV formulation (F4) showed 93.6% ± 0.36 entrapment efficiency, 97% ± 0.43 drug content, a vesicle size of 98.36 ± 2 nm, and a pH of 6.69 ± 0.76. F4 attained a drug release of 97.8% ± 0.72 after 24 h and markedly improved ex vivo skin permeability relative to an RIV suspension ( p < 0.05). F4 had a zeta potential of -24.16 mV and a deformability index of 9.6 ± 0.34. The absence of drug–excipient incompatibilities was confirmed by Fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), and powder X-ray diffraction (PXRD). Field-emission scanning electron microscopy (FESEM) demonstrated smooth, spherical vesicles. F4 demonstrated enhanced ex vivo skin permeation and suitable physicochemical characteristics.