Enhanced Anti Arthritic Potential of Tacrolimus by Transdermal Nanocarrier System

Abstract

Current work entails the development and assessment of a well-tolerated colloidal carrier system containing immunosuppressant drug tacrolimus (TL) for transdermal delivery to study its efficacy against arthritis. TL-NEs of different composition from phase diagram were prepared by high sheer homogenization and a comprehensive physico-chemical characterization of the novel NEs were performed using different techniques in order to get most optimum NE. Optimized NE was incorporated in to carbopol-934 gel and subjected to ex vivo skin permeation studies, droplet size analysis, zeta potential measurement, TEM examination, Rheology, and stability study. Moreover, we have evaluated the in vivo anti arthritic potential of same formulation and compared it with a marketed ointment (Protopic®, 0.03%) for the first time. Optimized TL-NG formulation composed of Capryol 90 (5.0% w/w), tween-20 (15.0% w/w), Transcutol HP (7.5% w/w), water (72.5%) w/w, carbopol-934 (1.0%) and found to have permeation flux (68.88 μg/cm2/h), release (1621.46 μg/24 h), small droplet size (12.72 nm), and viscosity of 1.07 Pa-s. The results of ZP indicated that formulation was stable and shelf life at room temperature was calculated as 1.59 years. The in vivo investigation demonstrated direct evidence on significant reduction (41.80%) in inflammation over a period of 24 h. On the basis of these preliminary finding, we conclude that developed TL-NG has good anti-inflammatory action and may provide promising perspective for treatment of Arthritis.