Metal-ion speciation in blood plasma incorporating the water-soluble polymer, polyethyleneimine functionalised with methylenephosphonate groups, in therapeutic radiopharmaceuticals

Abstract

Summary A water-soluble polymer, polyethyleneimine functionalised with methylene phosphonate groups (PEI-MP) and labelled with 99mTc, has shown selective uptake into bone tumours. Apparent formation constants for the complexation of important blood plasma metal-ions and metal-ions of radionuclides used in therapeutic radiopharmaceuticals (excluding Tc) with PEI-MP were measured potentiometrically. These were added to the ECCLES data base in order to construct a blood plasma model for PEI-MP. From this model it could be predicted that the polymer would not deliver the therapeutic radionuclides 153Sm, 166Ho, 212Pb, 213Pb and 89Sr to bone. This was clinically verified for 153Sm. However good uptake of 99mTc-PEI-MP could be demonstrated in dogs. Due to the similar chemistry of Re as compared to Tc, it can be expected that PEI-MP labelled with 186Re or 188Re could result in effective therapeutic radiopharmaceuticals for bone cancer.