Nanotechnology provides exciting opportunities for the development of novel, clinically relevant diagnostic and therapeutic multifunctional systems. Fluorescent carbon nanoparticles (CNPs) due to their intrinsic fluorescence and high biocompatibility are among the best candidates. As innovative nanomaterials, CNPs could be utilized both as nontoxic drug delivery system and bioimaging. We foresee a great future for CNPs in cancer diagnostic and therapy.