Rheumatoid arthritis (RA) is a chronic autoimmune inflammatory disease associated with persistent multiarticular synovitis, cartilage destruction, and even loss of joint function. Although remarkable progress has been made in the clinical treatment of RA, long-term administration of anti-rheumatic drugs still suffers quite a few drawbacks, including high dose and high frequency of drug use, as well as dysfunction of the heart, liver, kidney, and so forth. For the above problems, nanotherapeutic agents are developed to avert non-specific binding and upregulate the efficacy by improving the accumulation of drugs in lesion tissues. In this article, some of the most frequently used anti-RA agents were summarized, and the recent treatment of RA with passive or active targeting nanotheranostics was systematically illustrated. In addition, the prospect of nanovehicles in clinical therapy of RA was discussed and predicted. Display omitted