Nanocarriers are widely used for delivering drugs to tumors and are progressing in a stable trend, because malignant tumors remain a major health burden throughout the world and effective therapeutic strategies are urgently needed. Furthermore, as an integrated platform, nanocarriers have the potential to dramatically improve cancer diagnosis, imaging, and therapy, while reducing the toxicity associated with the current approaches. Significantly, intelligent nanocarriers are the new generation of the nanocarriers, exhibiting superior tumor targeting and improved therapeutic efficacy. In this review, we discuss recent development in the design of nanoscale stimuli-responsive systems which will be able to control drug biodistribution in response to specific stimuli, either exogenous or endogenous. Meanwhile, the recent progress in engineering intelligent and versatile nanomaterials for targeting the tumor microenvironment is summarized.
