We report the design and biological evaluation of a nanoplatform featuring controllable aggregation-induced emission (AIE) behavior. The free rotation of benzene rings (4-(1,2,2-triphenylvinyl) benzaldehyde) largely suppresses fluorescence in the pure organic phase. However, water-induced molecular aggregation enhances the fluorescence signal. The delivery system follows the membrane–cytoplasm–nucleus route and it leads to apoptosis in two cancer cells (U937 cells and Hela cells). The AIE moiety accumulates in the cytoplasm, emitting a bright-blue signal, but the anticancer drug doxorubicin selectively targets the nucleus with unique red emission. The current noninvasive method with DOX-triggered apoptosis holds promise for tumor diagnosis and real-time imaging.
