Tofacitinib (Tof), a JAK3 inhibitor, is clinically utilized for the treatment of moderate to severe rheumatoid arthritis (RA). However, long-term oral administration of Tof can lead to serious systemic toxicity and adverse effects. To mitigate its toxicity, this study prepared drug-loaded nanoparticles (NPs), PLGA@Tof, utilizing poly(lactic-co-glycolic acid) PLGA as the matrix. These NPs exhibited a particle size of 220 nm, a zeta potential of -13.4 mV, and a smooth spherical morphology. In vitro studies demonstrated that these NPs achieved sustained release of Tof without inducing hemolytic effects. Cellular experiments revealed that, compared to free Tof, drug-loaded NPs were more readily internalized by RAW264.7 cells under inflammatory conditions and exhibited enhanced reactive oxygen species (ROS) scavenging capabilities, as well as superior inhibition of inflammatory factors. These findings suggest that PLGA@Tof has the potential to be developed into a long-acting nanotherapeutic agent for systemic or localized injection in the treatment of RA.
Wang et al. (Fri,) studied this question.