Thyroid-associated ophthalmopathy (TAO) is an orbital inflammatory disease closely related to thyroid dysfunction and autoimmunity. The pathogenesis of TAO has not been fully elucidated yet. The conventional treatments have problems such as significant adverse reactions and high drug resistance rates. Through a systematic review of the research progress of Tripterygium wilfordii and its active components in the treatment of TAO from five aspects: theory, clinical practice, mechanism, clinical application safety, and nano-formulation, this paper explores the potential of Tripterygium wilfordii and its active components in treating TAO. The theoretical analysis shows that Tripterygium wilfordii’s functions of dispelling wind, removing dampness, relaxing muscles and tendons, and promoting blood circulation and relieving pain are in line with the pathogenesis of TAO, which involves liver depression, spleen deficiency, and blood stasis blocking the meridians. Clinical studies have confirmed that Tripterygium wilfordii alone or in combination with methimazole, prednisone, etc., can effectively improve the clinical symptoms of TAO patients. Mechanism research further reveals that the effects of Tripterygium wilfordii and its active components in treating TAO involve inhibiting inflammatory and immune responses, as well as anti-fibrotic effects, etc. In terms of clinical application safety, adverse reactions can be alleviated by adjusting dosage, formulation, processing methods, and compatibility. In terms of formulation improvement, the nano-delivery system, through targeted strategies, significantly enhances the targeted enrichment and therapeutic selectivity of active components of Tripterygium wilfordii in the lesion site, which is a key approach to achieving clinical enhancement of efficacy and reduction of toxicity. In summary, Tripterygium wilfordii and its active components show good potential in treating TAO in terms of theory, clinical practice, mechanism, and safety. Combined with modern nanotechnology and other formulation improvements, this may provide a promising new strategy for the traditional Chinese medicine prevention and treatment of TAO.

thyroid-associated ophthalmopathy  /  Tripterygium wilfordii Hook F.  /  immunosuppression  /  anti-inflammatory  /  anti-fibrotic  /  synergistic