Rheumatoid arthritis (RA) is a chronic autoimmune disorder characterized by persistent synovial inflammation and progressive joint destruction. While Tofacitinib, a Janus kinase (JAK) inhibitor, has emerged as an effective oral disease-modifying antirheumatic drug (DMARD), its systemic administration is often associated with suboptimal bioavailability, dose-related toxicity, and off-target effects. These challenges necessitate the development of advanced delivery strategies to enhance therapeutic efficacy while minimizing adverse effects.
Vesicular drug delivery systems such as liposomes, niosomes, ethosomes, transfersomes, and solid lipid nanoparticles (SLNs) offer promising platforms for targeted and controlled release of Tofacitinib. These nanocarriers can be engineered to improve drug encapsulation, increase stability, and facilitate site-specific delivery to inflamed joints via passive and active targeting mechanisms. Furthermore, their ability to cross biological barriers and achieve prolonged circulation enhances drug bioavailability and therapeutic index.
This review provides a comprehensive overview of the pharmacological profile of Tofacitinib, the rationale for vesicular systems in RA treatment, and the recent advances in vesicle-based Tofacitinib delivery. Preclinical data supporting the efficacy and safety of such systems are critically analyzed, alongside a discussion on formulation strategies, characterization techniques, and translational challenges. The integration of nanotechnology with JAK inhibition offers a forward-looking approach for the effective management of RA, with potential to reshape the therapeutic landscape.