Applications of nanoceria in the biomedical field are quite promising, as previous data has shown potential use of nanoceria as therapeutics via radical scavenging and oxidative stress mitigating properties. But, still, there are contradicting reports regarding nanoceria activity, mode of action, and in vitro toxicity in the cell. There are different nanoceria synthesis methods and Ligands for functionalization and loading of nanoceria into drugs for targeted drug delivery. Redox chemistry of nanoceria exerts their anticancer properties through apoptosis and oxidative stress as it can switch between Ce3+ and Ce4+ and act as free radical scavengers. For breast cancer treatment, cerium oxide nanoparticles (CeONPs) can act as protectant for healthy cells against on-going radiotherapy. Similarly, CeONPs were used to make pancreatic cancer cells more sensitive to radiation damage setting them on the apoptotic pathway. Herein, the study reflects the use of nanoceria as a drug delivery system in chemotherapy due to its efficiency in acidic pH and oxidase activity in the microenvironment. A controlled drug delivery system was adapted using a nano-complexes of AMD-GCCNP-DOX, which were then employed against the retinoblastoma cells from the human eye to target the overexpressing chemokine receptor 4 (CXCR4). In radiotherapy, nanoceria acts as radioprotectants due to their free radical scavenging property and inhibit the proliferation and migration of gastric cancer. This paper summarizes the synthesis methods and application of nanoceria in cancer.