Metal-ion speciation in blood plasma incorporating the bisphosphonate, 1-hydroxy-4-aminopropilydenediphosphonate (APD), in therapeutic radiopharmaceuticals.

Abstract:

:In the quest for more effective pain palliation radiopharmaceuticals for metastatic bone cancer, this paper relates results obtained with 166Ho complexed to the bone-seeking bisphosphonate, 1-hydroxy-4-aminopropililydenediphosphonate (APD). APD is itself a bone cancer pain palliation agent and this work was therefore driven by the idea that the energetic beta-particle emitter, 166Ho, coupled with APD could afford a highly effective radiopharmaceutical in the treatment of bone cancer. Complex-formation constants for important blood plasma metal-ions were measured by potentiometry or polarography at 37 degrees C and I = 150 mmol dm-3. The latter technique was used for systems where precipitates formed at ligand-to-metal ratios appropriate for potentiometry. For trivalent lanthanides, neither electrochemical technique could be used. Animal tests showed that the 166Ho-APD complex was taken up primarily by the liver due to precipitation or colloid formation.

journal_name

J Inorg Biochem

authors

Zeevaart JR,Jarvis NV,Louw WK,Jackson GE,Cukrowski I,Mouton CJ

doi

10.1016/s0162-0134(99)00027-6

subject

Has Abstract

pub_date

1999-04-01 00:00:00

pages

265-72

issue

4

eissn

0162-0134

issn

1873-3344

pii

S0162-0134(99)00027-6

journal_volume

73

pub_type

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