Receptor-mediated targeted drug or toxin delivery

Abstract

The new approach to the treatment of cancer or to immunomodulation is drug targeting. Cellular uptake of drugs bound to a targeting carrier or to a targetable polymeric carrier is mostly restricted to receptor-mediated endocytosis. Factors that influence the efficiency of receptor-mediated uptake of targeted drug conjugate are the affinity of the targeting moieties, the affinity and nature of the target antigen, density of the target antigen, the epitope of the target antigen, the type of cell target, the rate of endocytosis, the route of internalization of the ligand-receptor complex, the ability of the drug or toxin to release from its targeted carrier, the ability of the drug or toxin to escape from a vesicular compartment into the cytosol, the affinity of the carrier to the drug and the concentration of the carrier. Targeted chemotherapy is also significantly influenced by the antigenic modulation and/or immunoselection of tumor cells. The binding of drug (toxin) to targetable polymeric carrier considerably decreases unwanted side toxicity.