Rhenium-188 labelled meso-tetrakis[3,4-bis(carboxymethyleneoxy)phenyl] porphyrin for targeted radiotherapy: preliminary biological evaluation in mice.

Abstract:

PURPOSE:This study focusses on a promising carrier system for therapeutic and imaging purposes using meso-tetrakis[3,4-bis(carboxymethyleneoxy)phenyl] porphyrin (T(3,4)CPP). To assess its potential for clinical use, we labelled T(3,4)CPP with (188)Re and analysed some kinetic biodistribution parameters after intravenous injection in mice. MATERIALS AND METHODS:T(3,4)CPP was synthesized and labelled with (188)Re. Normal Kunming (KM) mice and melanoma- or hepatoma-bearing BALB/c nude mice were injected intravenously with 5.55 MBq (188)Re-labelled T(3,4)CPP and sacrificed at 0.5, 2, 4, and 24 h and 8, and 24 h, respectively. RESULTS:The (188)Re-T(3,4)CPP yield was more than 95% with specific activity 16.9 GBq (mol)(-1), and Vitamin C (VC) could increase its stability in vitro. In normal KM mice, (188)Re-T(3,4)CPP had fast blood clearance (approximately 99%, 24 h postinjection), low retention in the vital organs and hepatotropic characteristics. In nude mice, more than 4.4 and 6.1% uptake per gram of tumour (%ID g(-1)) at 8 h postinjection was in melanoma and hepatoma, respectively; this remained as high levels after 24 h as 4.6 and 6.5%, respectively. At 8 h, the tumour/blood and tumour/muscle (T/M) ratios in melanomas and hepatoma bearing mice were 7.3, 13,and 7.0, 20, respectively. Twenty-four hours later, these high ratios still continued in existence which were 9.6, 19 and 10, 25, respectively. CONCLUSION:The results obtained in this study indicate that (188)Re-T(3,4)CPP has better tumour affinity and retainable accumulation characteristics in carcinoma which can potentially be used for tumour-targeted radiotherapy.

authors

Jia ZY,Deng HF,Pu MF,Luo SZ

doi

10.1007/s00259-007-0682-0

subject

Has Abstract

pub_date

2008-04-01 00:00:00

pages

734-42

issue

4

eissn

1619-7070

issn

1619-7089

journal_volume

35

pub_type

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