Evaluation of multivalent, functional polymeric nanoparticles for imaging applications

Monica Shokeen, Eric D. Pressly, Aviv Hagooly, Alexander Zheleznyak, Nicholas Ramos, Ashley L. Fiamengo, Michael J. Welch, Craig J. Hawker, Carolyn J. Anderson

Research output: Contribution to journalArticlepeer-review

83 Scopus citations


A series of multivalent, functional polymer nanoparticles with diagnostic/imaging units and targeting ligands for molecular targeting were synthesized with the loading of the chain-end-functionalized GRGDS peptide targeting sequence (model system based on integrin αvβ 3) ranging from 0 to 50%. Accurate structural and functional group control in these systems was achieved through a modular approach involving the use of multiple functionalized macromonomer/monomer units combined with living free radical polymerization. In cellulo results show an increase in uptake in αvβ3 integrin-positive U87MG glioblastoma cells with increasing RGD loading and a possible upper limit on the effectiveness of the number of RGD peptides for targeting αvβ3 integrin. Significantly, this increased targeting efficiency is coupled with in vivo biodistribution results, which show decreased blood circulation and increased liver uptake with increasing RGD loading. The results demonstrate the importance of controlling ligand loading in order to achieve optimal performance for therapeutic and imaging applications for multivalent nanoparticle-based systems.

Original languageEnglish
Pages (from-to)738-747
Number of pages10
JournalACS nano
Issue number2
StatePublished - Feb 22 2011


  • cellular uptake
  • click chemistry
  • pharmacokinetics
  • polymeric nanoparticles


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