We have constructed a novel gated nanocarrier for the real-time monitoring of drug release, consisting of three parts: (i) mesoporous silica nanoparticles (MSNs) as the drug carrier, (ii) chitosan as the nanovalve to block and unlock the pores, and (iii) 1,8-naphthalimide fluorophore as a connecting arm and fluorescent signal source. In the absence of glutathione (GSH), the integrity of the system results in the formation of pores in a closed state and the sulfone would block the intramolecular charge transfer (ICT) process, leading to no fluorescence emission. However, the nucleophilic attack of GSH can cause the removal of the chitosan and recovery of ICT property, thus triggering drug release and green fluorescence emission. The results demonstrate that the change of GSH concentration in vivo or vitro would lead to a change in drug release as well as a concurrent change in fluorescence signal, which can expand the application of our gated nanocarrier for monitoring different drug release in real time.