Doxorubicin, one of the most effective antitumor drugs, causes serious adverse cardiac effects. As a derivative of tanshinone IIA, sodium tanshinone IIA sulfonate was exploited for curing cardiovascular disorders. The synergistic effect of the above drugs as a combination was investigated for treating cancer cells and attenuating myocardial apoptosis. A multicompartmentalized vesosome (MCV) was produced to co-deliver the drug combination. MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) assay and western blotting analysis demonstrated that the MCV can enhance the synergistic effect of the drug combination and promote the protection of STS in Dox-induced cardiomyocyte apoptosis.