Triptolide is one of the major active components of traditional Chinese Medicine (TCM) - Tripterygium wilfordii Hook. f. (TWHf), which has been reported to be effective in the treatment of patients with a variety of inflammatory and autoimmune diseases, especially rheumatoid arthritis. However, its clinical use is restricted due to its scarce water solubility and some toxic effects. In order to find innovative ways for administering triptolide and alleviating its disadvantages, the novel types of delivery systems have been developed. This paper reviews the studies of triptolide- loaded nano drug delivery systems (NDDS) in our group during the past three years. The preparation, characterization, pharmacology and toxicity of triptolide-loaded solid lipid nanoparticles, microemulsions and polymeric nanoparticles were investigated. The results indicated that the NDDS presented more powerful activity and a lower toxicity in comparison with common drug carrier.