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Radiochimica Acta

International Journal for chemical aspects of nuclear science and technology

Editor-in-Chief: Qaim, Syed M.

12 Issues per year

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Volume 99, Issue 11


In vivo 212Pb/212Bi generator using indium-DTPA-tagged liposomes

A. Le Du / M. Mougin-Degraef / E. Botosoa / A. Rauscher / A. Faivre Chauvet / Jacques Barbet / G. Montavon
Published Online: 2011-08-10 | DOI: https://doi.org/10.1524/ract.2011.1871


Indium-DTPA-tagged liposomes were studied in the present work as carriers of in vivo 212Pb/ 212Bi generator to be used in targeted alpha therapy. The liposomal uptake of 212Pb, into preformed liposomes, was investigated using different lipophilic chelate (DCP, 2,3-dimercapto-1-propanol (BAL), sodium acetate, and A23187), as a function of various parameters (temperature, concentrations of lipids, Pb, DTPA, ...) with 212Pb as a tracer. Different formulations of liposomes were tested to evaluate the radiolabeling efficiency. No complexing agent was necessary for the passage of Pb2+ through the membrane. It occurs naturally via a partial permeability of the lipid bilayer, which increases with the temperature. A complexing agent (DTPA) appears necessary to concentrate Pb in the internal compartment of the liposomes. Conditions were found (T=65 ºC, internal DTPA concentration of 0.025 M, pH 7.4, ...) yielding a high and rapid uptake of 212Pb in liposomes. The protocol established provides a novel method for the efficient entrapment of about 2–3 Pb atoms per liposome with a yield of 75% in conditions relevant for nuclear medicine.

Keywords: Liposomes; 212 Pb; 212Bi; Generator; Targeted alpha therapy

About the article

* Correspondence address: EMN/CNRS/IN2P3/ Université de Nantes, Laboratoire Subatech, 4 rue Alfred Kastler, BP 20722, 44300 Nantes, Frankreich,

Published Online: 2011-08-10

Published in Print: 2011-11-01

Citation Information: Radiochimica Acta International journal for chemical aspects of nuclear science and technology, Volume 99, Issue 11, Pages 743–749, ISSN (Print) 0033-8230, DOI: https://doi.org/10.1524/ract.2011.1871.

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