Pep2 peptide, a peptide ligand for CD36 (transmembrane glycoprotein or scavenger receptor B2), exhibits selective binding to CD36 over human serum albumin (HSA), IgG, and CD44 in cell-free assays at 1 mM concentration. Pep2 peptide-functionalized micelles, when loaded with the anticancer agent doxorubicin, significantly enhance the cellular uptake and cytotoxicity of doxorubicin in HepG2 hepatocellular carcinoma cells that overexpress CD36, compared to micelles without Pep2 peptide.