OBJECTIVE： To study the inhibitory effects of sinomenine （SIN）-loaded polylactic-co-glycolic acid-D-α-tocopherol polyethylene glycol 1000 succinate （PLGA-TPGS） nanoparticles （SPTN） on the proliferation of HCa-F cells in lymph tubes and ectopic transplantation tumors in mice. METHODS： HCa-F cell suspension were incubated with normal saline， 5-fluorouracil （FS）， sinomenine solutions （SS）， sinomenine PLGA nanoparticles （SPN） and SPTN， with concentration of 80 μg/ml. The cells were marked with CFSE， and then were injected with suspension 50 μl via one footpad of mice. Inhibitory effect of above suspensions on the proliferation of HCa-F in lymph tubes of mice was observed by fluorescence inverted microscope at 3， 6， 9， 12， 24 h （n＝15）. Mice were divided into normal control group， blank PLGA-TPGS nanoparticles （EPTN） group， normal saline group， SPTN group， SPN group， SS group and FS group with 10 mice in each group. The latter 5 groups were injected with relevant medicine 15 mg/kg， once a day， via tail vein for consecutive 10 days after the model of HCa-F cells-bearing ectopic transplantation tumor mice was established. The serum content of ALT， AST， γ-glutamyltransferase （γ-GT）， ALB and T-BIL were determined； solid tumors were taken， measured and weighed， and the inhibitory rate of tumor was also calculated. RESULTS： The inhibitory effect of above solution on the proliferation of HCa-F cells in descending order was as follows： SPTN＞SPN＞FS＞SS＞normal saline. Compared with normal saline group， the serum levels of ALT， AST， γ-GT and TBIL of SPTN group， SPN group， SS group and FS group decreased， while ALB level increased （P＜0.05）； the amount of tumor volume increase and tumor weight in SPTN group， SPN group and FS group decreased significantly （P＜0.05）. The inhibitory rate of tumor in 3 groups were 49.62％， 40.53％ and 33.90％. CONCLUSIONS： SPTN can inhibit the proliferation of HCa-F cells in lymph tubes of mice， and can improve HCa-F cells-bearing ectopic transplantation tumor in mice. It is better than SPN and FS.