After optimizing the composition of LNPs, a cathepsin B-cleavable prodrug (SMAC-P-FRRG-DOX) consisting of both second mitochondria-derived activator of caspases mimetic peptide (SMAC-P) and chemodrug (doxorubicin; DOX) was encapsulated into LNPs to form ApoLNPs that can induce potent apoptosis of targeted tumor cells in synergy of SMAC-P and DOX. Here, CTSB is linked to neoplasm.