Generation 5 poly(amidoamine) dendrimers were used as a nanoplatform to conjugate covalently an anticancer drug, alpha-tocopheryl succinate (α-Tos) and targeting ligand folic acid (FA). The formed multifunctional dendrimers are able to endow the hydrophobic drug α-Tos with improved water solubility for targeted inhibition of cancer cells via an FA receptor-mediated targeting pathway.