Rheumatoid arthritis (RA), a chronic autoimmune disease, is characterized by articular pain and swelling, synovial hyperplasia, and cartilage and bone destruction. Conventional treatment strategies for RA involve the use of anti-rheumatic drugs, which warrant high-dose, frequent, and long-term administration, resulting in serious adverse effects and poor patient compliance. To overcome these problems and improve clinical efficacy, drug delivery systems (DDS) have been designed for RA treatment. These systems have shown success in animal models of RA. In this review, representative DDS that target RA through passive or active effects on inflammatory cells are discussed and highlighted using examples. In particular, DDS allowing controlled and targeted drug release based on a variety of stimuli, intra-articular DDS, and transdermal DDS for RA treatment are described. Thus, this review provides an improved understanding of these DDS and paves the way for the development of novel DDS for efficient RA treatment.