Abstract
Both passive targeting and actively enhanced cellular internalization play significant roles in tumor-targeted therapy. Programmed specific targeting, as a novel targeting strategy that exploits stimuli-responsive structures, expects that nanocarriers show high stability during blood circulation for efficient passive targeting, then respond to tumor internal or external stimuli and transform into more cell-interactive forms upon arrival at the tumor tissue for enhanced cellular internalization. In this Perspective, we introduce recent advances in the design and development of stimuli-responsive programmed specific targeting nanomedicines, which are based on switchable surface charge, activatable targeting molecules, and variable coatings, to combine the advantages of passive targeting and actively enhanced cellular internalization.