The three batches of tetramethylpyrazine-loaded liposomes were prepared, and the properties ware as follows: the size of liposome was below 220 nm; Zeta electric potential was greater than 30 mV; the entrapment rates of them were 43.89%±3.88%, 61.23%±4.71% and 84.35%±6.67%, respectively. The inhibitation of tetramethylpyrazine and tetramethylpyrazine-loaded liposomes on VEGF gene in HUVEC cells were explored. The results proved that tetramethylpyrazine and tetramethylpyrazine-loaded liposomes had no effect on the proliferation of HUVEC, but regulated lower VEGF gene expression and inhibited angiogenesis. Tetramethylpyrazineloaded liposomes had lower effect than tetramethylpyrazine. Furthermore, the effects would be weakened with the increase of entrapment rate. It illustrat that the liposome is a novel preparation as the drug delivery for the slow release. It would be wide perspective for the application into the clinic in the future.