Treatment of rheumatoid arthritis by targeting macrophages through folic acid tailored superoxide dismutase and serratiopeptidase

Reactive oxygen species (ROS) released by activated macrophages causes oxidative stress, pain and inflammation and play a central role in causing inflammatory disorders like rheumatoid arthritis (RA). Thus therapeutics that can inhibit the production of ROS by macrophages has great clinical potential. Both Superoxide Dismutase (SOD) and Serratiopeptidase (STP) are dynamically involved in treating inflammatory diseases specifically RA by scavenging ROS and mitigating inflammation respectively. But, being protein these exhibit certain stability issues clinically. In the present study, both STP and SOD were individually conjugated with folic acid to target activated macrophages equipped with upregulated folate receptor during inflammatory stage. The experiments proved efficient conjugation of folic acid with both the enzymes and enhanced uptake of conjugated enzymes by macrophages with improved activity. Promising results obtained demonstrate enhanced potency and efficiency of both folate conjugated enzymes in future to treat RA and numerous related autoimmune disorders. (C) 2017 Elsevier B.V. All rights reserved.