We demonstrated that the albumin nanoparticles modified with dual ligands, a transferrin receptor (TfR)-binding peptide T12 and mannose, efficiently passed through the BBB via the nutrient transporters (i.e., TfR and the albumin-binding receptor SPARC) that were both overexpressed in the BBB and glioma cells, thus achieving biomimetic delivery to glioma. The gene discussed is TFRC; the disease is central nervous system cancer.