CASP3 and neoplasm: It confirmed that CTPP-CSOSA/Cela showed fast drug release in mitochondria with decreased drug leakage in the lysosome and cytoplasm, induced remarkably intensive ROS levels, had an enhanced accumulation in tumor tissue, and showed significant antitumor effect by decreasing mitochondrial membrane potential, promoting cytochrome c release, and upregulating caspase 3 and caspase 9.