Abstract: Tripterygium wilfordii Hook F (TWHF), specifically triptolide (TP), is an active compound derived from the plant with significant anti-rheumatoid arthritis (RA) effects. Studies show that TP exerts potent anti-inflammatory and antioxidant properties by inhibiting the expression of several inflammatory cytokines, such as TNF-α, IL-1β, and IL-6. In terms of immune regulation, TP modulates the activity of immune cells like T cells and neutrophils, reducing inflammation and tissue damage. Additionally, TP can regulate multiple signaling pathways, including NF-κB, JAK/STAT, and MAPK, to suppress the proliferation and invasion of synovial cells in RA, thereby mitigating joint damage. With the advancement of nanotechnology, the development of TP-based nanomedicine has gained attention in recent years. Innovative nanocarriers, such as polymer nanoparticles, exosomes, and inorganic nanoparticle drug delivery systems, have significantly improved TP's bioavailability and targeting capabilities while reducing its toxicity. By modifying the surface of these nanomaterials, their ability to target and release TP at inflammation sites is enhanced, leading to more precise drug delivery. Moreover, nanomedicines extend TP's circulation time in the body and reduce early-stage toxicity, thus improving the therapeutic outcomes for RA. In conclusion, TP and its nanomedicine formulations show great promise in RA treatment. Future research should continue to explore their mechanisms and clinical applications, offering new perspectives for the treatment of rheumatoid arthritis.