Abstract: In light of the high level of glutathione (GSH) in tumors, the study designed and prepared a novel glutathione (GSH)-responsive mesoporous silica nanoparticle (MSN) modified with cystamine dihydrochloride. The blockage of channels on the surfaces of MSN was achieved by the Schiff base reaction between amino groups in cystamine dihydrochloride and glutaraldehyde. The triggered release of drug was achieved by the cleavage of disulfide bond. Meanwhile, ibuprofen (IBU) and doxorubicin hydrochloride (DOX) were chosen as the model drugs to measure the loading capacity of the carrier and study the biocompatibility of carrier. Results showed that the release amount of the model drugs were well correlated with GSH concentration, and the functionalized MSN had good biocompatibility and phagocytosis ability.