Document Detail

Preparation and preliminary studies on 177Lu-labeled hydroxyapatite particles for possible use in the therapy of liver cancer.
MedLine Citation:
PMID:  18589303     Owner:  NLM     Status:  MEDLINE    
INTRODUCTION: Intra-arterial administration of particulates labeled with suitable beta(-)-emitting radionuclides has emerged as one of the most successful modality for the treatment of primary and metastatic liver cancer. (177)Lu [T(1/2)=6.73 d, E(beta)(max)=0.49 MeV, E(gamma)=208 keV (11%)] could be envisaged as a viable radionuclide for use in liver cancer therapy with wider acceptability owing to its feasibility of production in large-scale and relatively longer half-life providing logistic advantages. Hydroxyapatite (HA) particles of 20-60 microm size range are chosen as the particulate carrier due to its excellent biocompatibility and ease of labeling with lanthanides. METHODS: (177)Lu was produced by thermal neutron bombardment on enriched Lu target. HA particles of desired size range were synthesized and characterized. Radiolabeling of HA particles was achieved at room temperatures within 30 min. The biological behavior of (177)Lu-labeled HA particles prepared under optimized conditions was tested in Wistar rats. RESULTS: (177)Lu was produced with a specific activity of 444.2+/-41.8 GBq/mg and radionuclidic purity of 99.98%. (177)Lu-HA was prepared with high radiochemical purity of >99%, and the radiolabeled agent showed excellent in vitro stability. The agent exhibited approximately 73% retention of injected activity in liver after 14 days postadministration with insignificant uptake in any other major organ/tissue except skeleton in biodistribution and imaging studies. CONCLUSION: (177)Lu-HA exhibited promising features in radiochemical studies. However, preliminary biodistribution studies in normal Wistar rats exhibited suboptimum liver retention and an undesirable skeletal uptake.
Sudipta Chakraborty; Tapas Das; Haladhar D Sarma; Meera Venkatesh; Sharmila Banerjee
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Publication Detail:
Type:  Journal Article    
Journal Detail:
Title:  Nuclear medicine and biology     Volume:  35     ISSN:  0969-8051     ISO Abbreviation:  Nucl. Med. Biol.     Publication Date:  2008 Jul 
Date Detail:
Created Date:  2008-06-30     Completed Date:  2008-09-25     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  9304420     Medline TA:  Nucl Med Biol     Country:  England    
Other Details:
Languages:  eng     Pagination:  589-97     Citation Subset:  IM    
Radiopharmaceuticals Division, Bhabha Atomic Research Centre, Mumbai, India.
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MeSH Terms
Biocompatible Materials / chemical synthesis,  pharmacokinetics,  therapeutic use
Drug Carriers
Drug Stability
Durapatite / chemical synthesis*,  pharmacokinetics,  therapeutic use*
Image Processing, Computer-Assisted
Isotope Labeling
Liver Neoplasms / radionuclide imaging,  radiotherapy*
Lutetium / chemistry*,  pharmacokinetics,  therapeutic use*
Particle Size
Radiopharmaceuticals / chemical synthesis*,  pharmacokinetics,  therapeutic use*
Rats, Wistar
Tissue Distribution
Whole-Body Counting
X-Ray Diffraction
Reg. No./Substance:
0/Biocompatible Materials; 0/Drug Carriers; 0/Radioisotopes; 0/Radiopharmaceuticals; 1306-06-5/Durapatite; 7439-94-3/Lutetium

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