Tumor targeting, trifunctional dendritic wedge

Bioconjug Chem. 2015 Jan 21;26(1):78-89. doi: 10.1021/bc500436b. Epub 2014 Nov 12.

Abstract

We report in vitro and in vivo evaluation of a newly designed trifunctional theranostic agent for targeting solid tumors. This agent combines a dendritic wedge with high boron content for boron neutron capture therapy or boron MRI, a monomethine cyanine dye for visible-light fluorescent imaging, and an integrin ligand for efficient tumor targeting. We report photophysical properties of the new agent, its cellular uptake and in vitro targeting properties. Using live animal imaging and intravital microscopy (IVM) techniques, we observed a rapid accumulation of the agent and its retention for a prolonged period of time (up to 7 days) in fully established animal models of human melanoma and murine mammary adenocarcinoma. This macromolecular theranostic agent can be used for targeted delivery of high boron load into solid tumors for future applications in boron neutron capture therapy.

Publication types

  • Research Support, N.I.H., Extramural

MeSH terms

  • Animals
  • Biological Transport
  • Cell Line, Tumor
  • Cell Survival
  • Dendrimers / metabolism
  • Dendrimers / pharmacokinetics
  • Dendrimers / therapeutic use*
  • Humans
  • Integrins / metabolism
  • Ligands
  • Mice
  • Neoplasms / diagnosis*
  • Neoplasms / pathology
  • Neoplasms / therapy*
  • Tissue Distribution

Substances

  • Dendrimers
  • Integrins
  • Ligands