The invention relates to a multi-purpose cerium dioxide nanometer drug-loading system realizing the targeted stimulation responsiveness. According to the multi-purpose cerium dioxide nanometer drug-loading system, cerium dioxide with cytotoxicity is taken as a drug-loading main body, sugar is taken as a targeting group, the pillar [5] arene realizing sugar functionalization is taken as a host molecule, pyridinium salt modified on the surface of the cerium dioxide drug-loading main body and containing disulfide bonds is taken as a guest molecule, through the host-guest interaction, the pillar [5] arene realizing sugar functionalization is bonded to the surface of cerium dioxide adsorbing anti-cancer drug, and thus the anti-cancer drug is encapsulated to the surface of the drug-loading main body. Since the pillar arene containing galactosyls is connected to the surface, the biocompatibility of the system can be obviously improved; meanwhile, the galactosyls can act with specific galactose binding protein excessively expressed on the surfaces of cancer cells, so that the targeted selective entering into the cancel cells is realized, further, GSH with high concentration in the cancer cells is utilized for promoting disulfide bonds in the system to rapidly fracture, then the anti-cancer drug is released, the cerium dioxide nanometer particles with cytotoxicity are exposed out, and the synergy in resisting caner of the cerium dioxide nanometer particles and drug is realized.