Lipid nanodisks modified with folate (FA) were prepared and the cellular uptake was evaluated. FA-conjugated phospholipids were synthesized and incorporated into lipid nanodisks. Radiolabeled or fluorescently labeled FA-modified lipid nanodisks were efficiently taken up by human breast cancer MCF7 cells. The uptake was markedly inhibited in the presence of excess free FA, suggesting that the uptake was folate receptor-mediated. Our results demonstrated the potential of FA-modified lipid nanodisks as delivery vehicles for drugs or imaging agents.