Abstract: Drug delivery systems can facilitate the delivery of platinum-based drugs, enhance drug efficiency and protect Pt(Ⅳ) from being reduced before cellular uptake. A highly biocompatible Pt(Ⅳ) prodrugs delivery system using calcium phosphate (CaP) nanoparticles with simple preparation procedures were reported. The diameter and morphology of Pt(Ⅳ)/CaP nanoparticles were characterized by dynamic light scattering, scanning electron microscope and X-ray diffraction. Then cellular uptake efficiency and cytotoxicity were studied. The results indicate that nanoparticles are well-dispersive with narrow size distribution; they have high cellular uptake efficiency and redox response so as to release cisplatin after being reduced by cellular reductants. Moreover, the delivery system demonstrates a significantly higher inhibitory effect than the free Pt(Ⅳ) prodrug.