Cancer is a disease that shows uncontrolled cell division and invasion in other tissues, resulting in high incidence and mortality worldwide. Classical chemotherapeutic agents have poor water solubility and lack of specificity, resulting in systemic toxicity and limitations of the maximum drug dose. Alternatively, the use of nanosized drug carriers overcomes these drawbacks and increase therapeutic efficacy of many chemotherapy drugs. Nanocarriers for drug delivery allows systems to combine properties for multiple functions. Here, cyclodextrins are of particular interest due to their good inclusion capability, excellent biocompatibility, and ability to self-assemble and form various stable nanoscale systems such as micellar aggregates, nanoreservoirs and nanoparticles for biomedical applications. These cyclodextrin-based nanosystems show several advantages in terms of stability, safety, the ability to encapsulate hydrophobic drugs and good in vivo tolerance. Here we review cyclodextrin-based nanocarriers such as liposomes, nanoparticles, micelles for delivery of anticancer drugs in cancer therapy. We discuss preparation and characterization. We compare cyclodextrin-based nanocarrier groups for their potential in targeted delivery of anticancer agents such as chemotherapeutic drugs, and siRNA for cancer therapy or diagnosis. The major benefits are recognition of cancer cells and delivery of drugs to the target tissue, high antitumor efficacy and low adverse effects, prolonged blood circulation, higher drug loading, and controlled release. In vitro and in vivo studies performed in cell cultures and animal models have given promising results.