Synthesis and characterization of theranostic poly(HPMA)-c(RGDyK)-DOTA-64Cu copolymer targeting tumor angiogenesis: tumor localization visualized by positron emission tomography

Mol Imaging. 2013 May;12(3):203-12.

Abstract

Poly(HPMA)-c(RGDyK)-DOTA-64Cu copolymers were synthesized and characterized for tumor localization in vivo as a theranostic scaffold for cancer imaging and anticancer drug delivery targeting tumor angiogenesis. Tumor localization of the poly(HPMA)-c(RGDyK)-DOTA-64Cu copolymers was visualized in mice bearing human prostate cancer xenografts by positron emission tomography (PET) using a microPET scanner. PET quantitative analysis demonstrated that tumor 64Cu radioactivity (2.75 ± 0.34 %ID/g) in tumor-bearing mice 3 hours following intravenous injection of the poly(HPMA)-c(RGDyK)-DOTA-64Cu copolymers was significantly higher than the tumor 64Cu radioactivity (1.29 ± 0.26 %ID/g) in tumor-bearing mice injected with the nontargeted poly(HPMA)-DOTA-64Cu copolymers (p = .004). The poly(HPMA)-c(RGDyK)-DOTA-64Cu copolymers hold potential as a theranostic scaffold for cancer imaging and radiochemotherapy of prostate cancer targeting tumor angiogenesis by noninvasive tracking with PET.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Copper Radioisotopes / chemistry*
  • Heterocyclic Compounds, 1-Ring / chemistry*
  • Humans
  • Male
  • Methacrylates / chemistry*
  • Mice
  • Neovascularization, Pathologic / diagnosis*
  • Polymers / chemical synthesis*
  • Polymers / chemistry
  • Positron-Emission Tomography / methods*
  • Prostatic Neoplasms / diagnosis*

Substances

  • Copper Radioisotopes
  • Heterocyclic Compounds, 1-Ring
  • Methacrylates
  • Polymers
  • 1,4,7,10-tetraazacyclododecane- 1,4,7,10-tetraacetic acid
  • hydroxypropyl methacrylate