Lipoproteins are natural nanosized delivery vehicles within the circulatory system of all mammals. Scientists have long been interested in utilizing these endogenous macromolecules to transport exogenous imaging or therapeutic agents to specific cells or tissues in the body. The broad distribution of lipoprotein receptors throughout the body however has limited the utility of this approach for targeted delivery of medicinal agents. In recent years lipoprotein rerouting strategies have been developed wherein lipoproteins can be redirected from their natural lipoprotein receptors to an alternate receptor of choice. In this chapter we describe the basic methods of preparing folic acid-conjugated high-density lipoprotein nanoparticles for targeted delivery of imaging or chemotherapeutic agents to ovarian cancer cells.