These stimuli-switchable nanoparticles coated with the cleavable outer polymer coatingmultifunctional peptides may afford a new platform for anticancer drugmiR. These nanoparticles possess characteristics of environmental response, active targeting,gene/chemo combinatorial therapeutics, thus providing spatiotemporal control of posttranscriptional gene regulation, smart nuclear/mitochondrial localization,simultaneous inhibition of multiple progression pathways of tumor cells for enhancing antitumor efficacysafety of cancer therapy.