Abstract: The orthogonal design was used to optimize the inclusion of deoxypodophyllotoxin with sulphobutyl ether-β-cyclodextrin,and the prepared solid inclusion complex was confirmed by differential scanning calorimetry and X-ray diffration.After being included,the solubility of deoxypodophyllotoxin in water increased from 0.5 mg/L to 5 g/L.This solid inclusion complex was tested for in vitro and in vivo reveal antitumor activities,and the reslts revealed that this complex exhibited significant antitumor activity against various cancer cell lines.