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In vivo tumor targeting by a NGR-decorated micelle of a recombinant diblock copolypeptide.

Publication ,  Journal Article
Simnick, AJ; Amiram, M; Liu, W; Hanna, G; Dewhirst, MW; Kontos, CD; Chilkoti, A
Published in: J Control Release
October 30, 2011

Antivascular targeting is a promising strategy for tumor therapy. This strategy has the potential to overcome many of the transport barriers associated with targeting tumor cells in solid tumors, because the tumor vasculature is directly accessible to targeting vehicles in systemic circulation. We report a novel nanoscale delivery system consisting of multivalent polymer micelles to target receptors that are preferentially upregulated in the tumor vasculature and perivascular cells, specifically CD13. To this end we utilized amphiphilic block copolymers, composed of a genetically engineered elastin-like polypeptide (ELP) that self-assemble into monodisperse spherical micelles. These polymer micelles were functionalized by incorporating the NGR tripeptide ligand, which targets the CD13 receptor, on their corona. We examined the self-assembly and in vivo tumor targeting by these NGR-functionalized nanoparticles and show that multivalent presentation of NGR by micelle self-assembly selectively targets the tumor vasculature by targeting CD13. Furthermore, we show greater vascular retention and extravascular accumulation of nanoparticles in tumor tissue compared to normal tissue, although the enhancement is modest. These results suggest that enhanced delivery to solid tumors can be achieved by targeting upregulated receptors in the tumor vasculature with multivalent ligand-presenting nanoparticles, but additional work is required to optimize such systems for multivalent targeting.

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Published In

J Control Release

DOI

EISSN

1873-4995

Publication Date

October 30, 2011

Volume

155

Issue

2

Start / End Page

144 / 151

Location

Netherlands

Related Subject Headings

  • Xenograft Model Antitumor Assays
  • Temperature
  • Scattering, Radiation
  • Reverse Transcriptase Polymerase Chain Reaction
  • Pharmacology & Pharmacy
  • Peptides
  • Oligopeptides
  • Neovascularization, Pathologic
  • Microscopy, Fluorescence
  • Microscopy, Confocal
 

Citation

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Simnick, A. J., Amiram, M., Liu, W., Hanna, G., Dewhirst, M. W., Kontos, C. D., & Chilkoti, A. (2011). In vivo tumor targeting by a NGR-decorated micelle of a recombinant diblock copolypeptide. J Control Release, 155(2), 144–151. https://doi.org/10.1016/j.jconrel.2011.06.044
Simnick, Andrew J., Miriam Amiram, Wenge Liu, Gabi Hanna, Mark W. Dewhirst, Christopher D. Kontos, and Ashutosh Chilkoti. “In vivo tumor targeting by a NGR-decorated micelle of a recombinant diblock copolypeptide.J Control Release 155, no. 2 (October 30, 2011): 144–51. https://doi.org/10.1016/j.jconrel.2011.06.044.
Simnick AJ, Amiram M, Liu W, Hanna G, Dewhirst MW, Kontos CD, et al. In vivo tumor targeting by a NGR-decorated micelle of a recombinant diblock copolypeptide. J Control Release. 2011 Oct 30;155(2):144–51.
Simnick, Andrew J., et al. “In vivo tumor targeting by a NGR-decorated micelle of a recombinant diblock copolypeptide.J Control Release, vol. 155, no. 2, Oct. 2011, pp. 144–51. Pubmed, doi:10.1016/j.jconrel.2011.06.044.
Simnick AJ, Amiram M, Liu W, Hanna G, Dewhirst MW, Kontos CD, Chilkoti A. In vivo tumor targeting by a NGR-decorated micelle of a recombinant diblock copolypeptide. J Control Release. 2011 Oct 30;155(2):144–151.
Journal cover image

Published In

J Control Release

DOI

EISSN

1873-4995

Publication Date

October 30, 2011

Volume

155

Issue

2

Start / End Page

144 / 151

Location

Netherlands

Related Subject Headings

  • Xenograft Model Antitumor Assays
  • Temperature
  • Scattering, Radiation
  • Reverse Transcriptase Polymerase Chain Reaction
  • Pharmacology & Pharmacy
  • Peptides
  • Oligopeptides
  • Neovascularization, Pathologic
  • Microscopy, Fluorescence
  • Microscopy, Confocal