Sirolimus-loaded poly (lactic acid-co-glycol acid) (PLGA) films were prepared by a casting method. 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay was performed to determine the optimal concentration of sirolimus for vascular smooth muscle cell (VSMC) inhibition effect. Based on the results of MTT, three samples of different weight percent loaded-sirolimus (2wt%, 6wt%, 15wt%) PLGA films were selected. The release of lactate dehydrogenase (LDH) was used to evaluate the immediate toxicity of the sirolimus-loaded PLGA films and it was shown that the three different concentrations of sirolimus-loaded films have low toxicity. Alamar blue results indicate that the sirolimus-loaded films have better antiproliferation effect than 316 stainless steel (SS). The higher the sirolimus concentration in the film is, the better is the antiproliferation effect. These films may be used for stent coating to inhibit in-stent restenosis induced by VSMC proliferation.