Fabrication of cRGD-Conjugated Dual-Responsive Micelles to Target αvβ5 Integrin-Overexpressed Cancer

  • Huacheng He
  • Remant Bahadur K.C.
  • Peisheng Xu
Part of the Methods in Pharmacology and Toxicology book series (MIPT)


Decoration of nano-sized carriers with targeting ligands facilitates their cellular uptake in specific cells due to the ligand-receptor interaction and is being widely applied to fabricate nanoparticles for tumor-targeted therapy. In this chapter, we describe a strategy to covalently attach cyclo(Arg-Gly-Asp-D-Phe-Cys)(cRGD) peptide to a pH and redox potential dual-responsive micelle to realize tumor targeting. The micelle formation is based on the self-assembly of an amphiphilic polymer. The synthesis of the polymer and its post-modification including PEG-SH grafting and cRGD conjugation are comprehensively described. The fabrication of micelles and the investigation of its responsiveness to pH and redox potential are further introduced. Finally, the study of the targeting effect of cRGD micelles to αvβ5 integrin-overexpressed HCT 116 cells is also described.


Conjugate cRGD Integrin Micelle Polymer Responsive Stimuli Target Tumor therapy 



This work is supported by the ASPIRE award from the Office of the Vice President for Research of the University of South Carolina, and the Center for Targeted Therapeutics (1P20GM109091-01) from National Institutes of Health (NIH).


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Copyright information

© Springer Science+Business Media New York 2015

Authors and Affiliations

  1. 1.Department of Drug Discovery and Biomedical Sciences, South Carolina College of PharmacyUniversity of South CarolinaColumbiaUSA

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