Targeted dendrimers for cancer diagnosis and therapy

An ideal anticancer drug must be able to distinguish cancer cells from healthy ones and provide a sufficiently high dose of toxic contents to kill the cancer cells. This chapter discusses the applications of targeted dendrimers as cancer diagnostics and therapeutics. The ligands modified on dendrimers for cancer targeting include low molecular weight ligands such as folic acid, carbohydrate, biotin, riboflavin, estrogen, and macromolecular ligands such as antibodies, peptides, transferrin (Tf), lactoferrin (Lf), growth factors, and aptamer. This chapter shows the targeting mechanisms and efficacies of ligand-modified dendrimers. It describes peptide-modified dendrimers include arginine-glycine-aspartate (RGD), luteinizing hormone-releasing hormone (LHRH), and several brain-targeting peptides. The diagnostic methods include computed tomography (CT), single-photon emission computed tomography (SPECT), magnetic resonance imaging (MRI), and near-infrared (NIR) fluorescence imaging. Dendrimers can also be used for signal amplification in the in vitro analysis of cancer biomarkers or as scaffolds for in vivo diagnosis of cancer.