Development And Evaluation Of Baricitinib -Gel Loaded Transdermal Patches For Treatment In Rheumatoid Arthritis

Abstract

Objectives: The study aimed to develop and optimize a baricitinib-loaded transdermal gel-patch system for enhanced delivery in rheumatoid arthritis management, improving drug release, skin permeability, and therapeutic efficacy.

Methods: A transdermal gel was formulated using Carbopol 940P and propylene glycol, and optimized using a 3² full factorial design. Evaluations included physicochemical characterization, ex vivo permeation, in vitro drug release, FTIR and DSC compatibility studies, and in vivo anti-arthritic activity in a CFA-induced rat model. The optimized gel was incorporated into a patch system and assessed for mechanical and stability parameters.

Results: The optimized formulation (F9) exhibited desirable viscosity (3789 ± 165 cP), spreadability (1.6 ± 0.09 cm), drug content (98.8 ± 1.1%), and gel strength (312 ± 16 g). Batch F9 demonstrated the highest sustained drug release (94.8 ± 3.0% at 12 h) (Figure 4). The selected optimized patch (GT3) showed a steady-state flux of 21.5 ± 1.2 μg/cm²/h and 66.9 ± 2.8% drug release at 12 h (Figure 6), with improved folding endurance and adhesion strength (445 ± 25 and 0.94 ± 0.06 N/cm², respectively). In vivo studies confirmed superior arthritis score reduction (7.2 ± 1.2), 60.8% paw volume inhibition, improved hematological and cytokine profiles, and weight recovery. GT3 remained stable over 6 months under accelerated conditions (Table 12).

Conclusion: The optimized baricitinib-loaded gel patch (GT3) demonstrated sustained release, enhanced permeability, and effective anti-arthritic activity, indicating strong potential for clinical translation in chronic inflammatory conditions like rheumatoid arthritis.