Advances in strategies to improve drug delivery to brain tumors.

Brain tumors remain a significant health problem. Advances in the biology of the blood-brain barrier are improving the ability of researchers to target therapeutic peptides, small molecules and other drugs to brain tumors. Simple methods to improve blood-brain barrier penetration include chemical modification, glycosylation and pegylation. Drug-delivery vehicles, such as nanoparticles and liposomes, are also under study. Targeting vectors include natural ligands (e.g., epidermal growth factor) or monoclonal antibodies to receptors (e.g., transferrin or insulin). Other vector-mediated delivery approaches involve the conjugation of a therapeutic peptide or protein with a targeting molecule that can induce transcytosis across blood-brain barrier endothelial cells. The most commonly used vectors are peptidomimetic antibodies to endothelial receptors, such as the transferrin and insulin receptors.