Objective: To optimize the preparation process of curcumin-hydroxypropyl-β-cyclodextrin(CUR-HP-β-CD) inclusion complex and to evaluate its in vitro antitumor activity. Method: CUR-HP-β-CD inclusion complex was prepared by the procedure of ethanol-water cosolvent incubation-lyophilization;the preparation technology was optimized by orthogonal test with inclusion rate as index.CUR-HP-β-CD inclusion complex was characterized by ultraviolet spectrophotometry(UV) and fluorescence spectrophotometry.The cell viability of different types of cancer cells(human cervical cancer cell line HeLa cells and human hepatoma cell line HepG2 cells) was measured by microculture tetrazolium(MTT) assay through exposing cells to different concentrations of CUR-HP-β-CD inclusion complex for different times(24 h and 48 h). Result: The optimum process for preparation of CUR-HP-β-CD was as follows:the molar ratio of CUR to HP-β-CD of 1:3

the cosolvent ratio (absolute ethanol-water) of 1:9

the reaction temperature at 40℃ and the reaction time for 12 h;under these conditions

the inclusion rate was 42.2%

its lyophilized product had formed CUR-HP-β-CD inclusion complex.Both CUR-HP-β-CD inclusion complex and free CUR reduced the viability of HeLa and HepG2 cells in a dose-dependent manner

and their half-inhibitory concentrations were close

showing that CUR-HP-β-CD inclusion complex still exhibited significant cytotoxicity to cancer cells. Conclusion: The optimized technique is simple and reproducible.Besides

CUR-HP-β-CD inclusion complex retains the bioactivity of CUR.