Biologically targeted nanoparticles as cancer therapeutics

The concept of biological targeting has led to the development of a new generation of therapeutic agents. These molecularly targeted agents have achieved great clinical results not previously seen with conventional agents. Their success, in turn, has inspired the development of biologically targeted nanoparticles for therapeutic applications, especially for the treatment of cancers. Biologically targeted nanoparticles are engineered by functionalizing the nanoparticles' surface with targeting ligands, such as antibodies, peptides, small molecules and oligonucleotides. Targeting ligands can improve the differential accumulation of nanoparticles at specific sites in the diseased tissue. Preclinical data have demonstrated that targeted nanoparticles are more efficacious and less toxic when compared to non-targeted nanoparticles. In this chapter, we will review the rationale for molecularly targeting nanoparticles, overview the various classes of targeting ligands, discuss the formulation of targeted nanoparticles, and highlight interesting examples from the preclinical data on targeted nanoparticle therapeutics.