Here,we report a strategy to deliver drug nanoparticles into cells with nucleus-targeting ability under a spatiotemporal control.The nanoparticles were constructed through self-assembly of photoresponsive prodrugs and free drugs.By incorporating a nucleus localization sequence in the system,drug nanoparticles could be delivered into nuclei upon visible light irradiation.The drug nanoparticles showed high drug loading capacity and specific nucleus-targeting ability,which efficiently killed cancer cells.This self-assembly strategy could be applied to other hydrophobic drugs and targeting ligands for photo-controlled organelle-targeted drug delivery.