Objective: To investigate the in vivo and in vitro antitumor activity of nanostructured lipid carriers of dihydroartemisinin(DHA-NLC).Methods: The inhibition effects of DHA-NLC and DHA suspension on solid tumor growth were evaluated in tumor-bearing mice with evaluation criterion of the inhibition rate.MTT assay was used to detect proliferation activity on human leukemia cells(K562),human leukemia multidrug resistance cell line K562 / ADM(KA) and glioma cells(U87).Results: DHA-NLC significantly inhibited tumor growth at 20,40 and 80 mg·kg-1,and the inhibition rates were 74.43%,81.13%,88.70% and 64.93,74.55,and 82.37%,respectively.DHA-NLC obviously inhibited cell proliferation in K562,KA and U87 cells,which was positively related to the time and concentration(P 0.05).Inhibition rates of DHA-NLC on proliferation of K562KA and U87 cells were significantly higher than those of dihydroartemisinin ordinary suspension at the same concentration.Conclusion: DHA-NLC has significant antitumor effect.