Cancer is one of the leading causes of mortality worldwide. Chemotherapy, radiation, and surgical resection are common forms of traditional treatment. However, these medicines provide a slew of toxicity issues for patients, owing to their non-selectivity, which leads to drug resistance and significant side effects. In this light, nanotechnology has been promoted as a smart technology that allows the system to focus medications in specific locations. Various nanomaterials that are commonly employed as a drug-delivery vehicle are produced for biomedical purposes using nanotechnology. Mesoporous silica nanoparticles (MSNs) have attracted a lot of attention because of their structural properties, large surface areas, tunable pore diameters, good thermal and chemical stability, excellent bio compatibility, and ease of surface modification. Furthermore, drug release from MSNs can be controlled via a variety of stimulusresponse gatekeeper systems. The organized structure of MSNs is particularly appropriate for loading a large number of drug molecules with regulated delivery for targeting cancer tissues via improved permeability and retention effect or additional surface modification, and it may also be actively targeted by different ligands. Although MSNs are becoming a potential tool for more efficient and safer cancer therapy, further translational research is needed to investigate their multifunctional capabilities in a clinical environment.