Ru(II) polypyridyl complexes are compounds of great interest in cancer therapy due to their unique photophysical, photochemical, and biological properties. For effective treatment, they must be able to penetrate tumor cells effectively and selectively. The development of nanoscale carriers capable of delivering Ru(II) polypyridyl complexes has the potential to passively or selectively enhance their cellular uptake in tumor cells. Many different strategies have been explored to incorporate Ru(II) polypyridyl complexes into a variety of nanosized constructs, ranging from organic to inorganic materials. Herein, recent developments in nanomaterials loaded with Ru(II) polypyridyl complexes are highlighted. Their rational design, preparation, and physicochemical properties are described, and their potential applications in cancer therapy are eventually discussed.