Integrin Targeted Delivery of Chemotherapeutics

• Main Author: Kai Chen, Xiaoyuan Chen
• Format: Article
• Language: English
• Published: Ivyspring International Publisher 2011-01-01
• Series: Theranostics
• Online Access: http://www.thno.org/v01p0189.htm

<p>Targeted delivery of chemotherapeutics is defined in the sense, that is, to maximize the therapeutic index of a chemotherapeutic agent by strictly localizing its pharmacological activity to the site or tissue of action. Integrins are a family of heterodimeric transmembrane glycoproteins involved in a wide range of cell-to-extracellular matrix (ECM) and cell-to-cell interactions. As cell surface receptors, integrins readily interact with extracellular ligands and play a vital role in angiogenesis, leukocytes function and tumor development, which sets up integrins as an excellent target for chemotherapy treatment. The peptide ligands containing the arginine-glycine-aspartic acid (RGD), which displays a strong binding affinity and selectivity to integrins, particularly to integrin &#945;v&#946;3, have been developed to conjugate with various conventional chemotherapeutic agents, such as small molecules, peptides and proteins, and nanoparticle-carried drugs for integtrin targeted therapeutic studies. This review highlights the recent advances in integrin targeted delivery of chemotherapeutic agents with emphasis on target of integrin &#945;v&#946;3, and describes the considerations for the design of the diverse RGD peptide-chemotherapeutics conjugates and their major applications.</p>