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Rheumatoid arthritis (RA) is a widespread autoimmune inflammatory disease. It implicates damage to bones, cartilage, and joints with uncertain pathogenesis. It is coupled with an elevated risk of cardiovascular complications and human disability. The conventional dosage forms for RA treatment pose numerous problems including poor efficacy, large dosages, frequent administration, limited responsiveness, greater expenses, and severe side effects. The nanoparticulate systems are emerging as a new thought for the diagnosis and treatment of RA. Anti-inflammatory drug-loaded nanoparticulate systems aid in the active and passive targeting of the inflamed region. Improved bioavailability and targetability are achieved by using these systems. In this review, the pathophysiology of RA and its conventional treatment has been discussed. The role of various nanoparticulate systems for passive and active targeting of RA has been reviewed. The authors have summarized the current practices in the typical and novel nanosystems to improve the quality of life in RA patients.