The nanotechnology approach has been recently adopted to provide more reliable, effective, controlled, and safe drug delivery systems. Nanostructured materials have gained great interest, including siliceous and carbonaceous nanoparticles. The effectiveness of mesoporous carbon nanoparticles (MCNs) in tumor imaging, targeting, and treatment is urging for more future studies. MCNs possess superior properties such as their biocompatibility, large surface area, large pore volume, tunability, and more responsive behavior to internal and external release triggers. These outstanding features make MCNs more applicable for stimuli-responsive drug delivery than the conventional forms of mesoporous silica nanoparticles (MSNs) and other carbon nanoparticles. In this review, we outlined the latest updates regarding the safety, benefits, and potential applications of MCNs.