Self-fluorescent and stimuli-responsive drug nanocarriers were developed based on curcumin gatekeeper on a platform of mesoporous silica nanoparticles with large pores (named LP) for drug delivery. The cur cumin gatekeeper was anchored to the surface of LP via thiol-ene "click" chemistry, and the pluronic polymer, F127, was coated to the out surface of the nanocarrier by self-assembly through hydrophobic interactions to provide a hydrophobic micro-environment and to improve the dispersity of the nanoparticles. In vitro drug release profiles indicated that curcumin can be confined in the pores in absence of GSH at pH 7.4. In the presence of GSH and at pH 5.5 condition, the beta-thioesters were hydrolyzed leading to curcumin release. Further investigations show that the curcumin gatekeeper can be served as fluorescent agent to avoid the use of other fluorescent label. This novel drug nanocarriers will inspire the development of new smart and self-fluorescent drug nanocarriers with imaging and therapeutic goals for cancer therapy. (C) 2016 Elsevier B.V. All rights reserved.