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Gjermund Henriksen, B. W. Schoultz, P. Hoff, R. H. Larsen

Potential in vivo generator for alpha-particle therapy with ²¹²Bi: Presentation of a system to minimize escape of daughter nuclide after decay of ²¹²Pb to ²¹²Bi

Radiopharmaceuticals based on ²¹²Pb (t_1/2=10.6h) are of interest for use as an in vivo generator of α-particle emitting ²¹²Bi (t_1/2=60.6min). Sterically stabilized liposomes were evaluated as carriers of ²¹²Pb/ ²¹²Bi radionuclides in the reported study. ²¹²Pb/ ²¹²Bi-containing vesicles were prepared by ionophore mediated loading of ²¹²Pb into preformed liposomes. The liposomal uptake of ²¹²Pb with or without various concentrations of lead carrier was investigated. The retention of ²¹²Pb and ²¹²Bi in liposomes incubated in serum was studied. Conditions were found yielding a high and rapid uptake of ²¹²Pb in liposomes. 90&plusm;2 of ²¹²Pb was incorporated after 30min. The retention of radionuclides was high, 95 of ²¹²Pb and ²¹²Bi were retained in liposomes after incubating for 20h at 37°C in serum. The results from the present work indicate that an effective retention of ²¹²Bi after the β^--decay of ²¹²Pb is achievable. This technology could be the basis of α-emitting radiopharmaceuticals built upon ²¹²Pb.

Radiochimica Acta, Oldenbourg Wissenschaftsverlag

Print ISSN: 0033-8230
Volume: 91, 02/2003
Pages: 109

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