Abstract: The preparations of Tripterygium wilfordii Hook F. have been widely used for the treatment of autoimmune and inflammatory diseases， and they show excellent curative effects in attenuating rheumatoid arthritis， glomerulonephritis and cancers. Triptolide (TPL) was determined as the primary biologically active ingredient of Tripterygium wilfordii. However， it shows high toxicity， poor water solubility， and narrow therapeutic window， which greatly limits its clinical applications. It was reported that the toxicity of triptolide originated from the mechanism of its medicinal effect， thus conventional structural modification was difficult to improve its druggability. Therefore， how to reduce the toxicity and increase the efficacy of triptolide is a problem needs to be solved urgently. It is expected to solve the problem of poor druggability of triptolide by improving water solubility and targeted delivery through the strategy of prodrug design.