Synthesis of Poly[APMA]-DOTA-Cu Conjugates for Interventional Radionuclide Therapy of Prostate Cancer: Assessment of Intratumoral Retention by Micro–Positron Emission Tomography
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(isobutyronitril...
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| Main Authors: | , , , , , |
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| Format: | Article |
| Language: | English |
| Published: |
SAGE Publishing
2007-01-01
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| Series: | Molecular Imaging |
| Online Access: | https://doi.org/10.2310/7290.2006.00030 |
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| Summary: | 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 ( M n 5 2.40 × 10 4 , M w / M n = 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 64 Cu radionuclide. Prolonged retention of poly[APMA]-DOTA- 64 Cu 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- 64 Cu conjugates might be useful for interventional radionuclide therapy of locally recurrent prostate cancer in humans. |
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| ISSN: | 1536-0121 |