Integrin Targeting Using RGD-Based Peptide Amphiphiles

  • Poonam Saraf
  • Xiaoling Li
  • Bhaskara Jasti
Part of the Methods in Pharmacology and Toxicology book series (MIPT)


Active targeting has been explored for improving accumulation of drugs at the tumor site via specific ligand receptor interactions. The tripeptide “Arg-Gly-Asp” or RGD has shown tremendous potential as a targeting ligand in improving the delivery of drugs and diagnostic agents to integrin-overexpressing tumors. The different integrin-based targeting drug delivery systems studied include polymeric nanoparticles, polymeric micelles, and dendrimers, most of which are prepared by decorating RGD ligand on the surface of the drug delivery system. Our group previously reported the potential of peptide-based amphiphiles for integrin targeting of hydrophobic drugs. These amphiphiles are built by solid-phase peptide synthesis and contain RGD as the hydrophilic head group (also as a targeting ligand), a fatty acid as lipid tail and multiple units of hydrophilic linker. The focus of this chapter is to outline methodologies used for the synthesis, characterization, and evaluation of these low-molecular-weight RGD-based micellar carriers for delivery of hydrophobic anticancer agents. The experimental details and factors to be considered for optimal methods are discussed.


Targeting RGD Peptide amphiphile Micelles 


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Copyright information

© Springer Science+Business Media New York 2015

Authors and Affiliations

  1. 1.Department of Pharmaceutics and Medicinal Chemistry, Thomas J. Long School of Pharmacy and Health SciencesUniversity of the PacificStocktonUSA

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