Synthesis of poly[APMA]-DOTA-64Cu conjugates for interventional radionuclide therapy of prostate cancer: Assessment of intratumoral retention by micro-positron emission tomography

Jianchao Yuan, Yezi You, Xin Lu, Otto Muzik, David Oupicky, Fangyu Peng

Research output: Contribution to journalArticle

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Abstract

To develop new radiopharmaceuticals for interventional radionuclide therapy of locally recurrent prostate cancer, poly[N-(3-aminopropyl)methacrylamide] [poly(APMA)] polymers were synthesized by free radical precipitation polymerization in acetonedimethylsulfoxide using N,N-azobis(isobutyronitrile) as the initiator. The polymers were characterized with nuclear magnetic resonance, size exclusion chromatography, and dynamic light scattering (Mn = 2.40 × 104, Mw/Mn = 1.87). Subsequently, poly[APMA] was coupled with 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA) using 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride as an activator, followed by conjugation with 64Cu radionuclide. Prolonged retention of poly[APMA]-DOTA-64Cu conjugates within the tumor tissues was demonstrated by micro-positron emission tomography at 24 hours following intra-tumoral injection of the conjugates to human prostate xenografts in mice. The data suggest that the poly[APMA]-DOTA-64Cu conjugates might be useful for interventional radionuclide therapy of locally recurrent prostate cancer in humans.

Original languageEnglish (US)
Pages (from-to)10-17
Number of pages8
JournalMolecular Imaging
Volume6
Issue number1
DOIs
StatePublished - Jan 1 2007

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ASJC Scopus subject areas

  • Biotechnology
  • Molecular Medicine
  • Biomedical Engineering
  • Radiology Nuclear Medicine and imaging
  • Condensed Matter Physics

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