Nanotechnology has been extensively utilized in the design and development of powerful strategies for drug delivery and cancer theranostic. Nanoplatforms as a drug delivery system have many advantages such as imaging, combined drug delivery, extended circulation time, and systemic controlled release. The functional biomimetic drug delivery could be realized by incorporating stimuli-responsive (pH, temperature, redox potential, etc.) properties into the nanocarrier system, allowing them to bypass biological barriers and arrive at the targeted area. In this review, we discuss the role of internal stimuli-responsive nanocarrier system for imaging and drug delivery in cancer therapy. The development of internal stimuli-responsive nanoparticles is highlighted for precision drug delivery applications, with a particular focus on imaging, drug release performance, and therapeutic benefits.