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Radiopharmaceuticals based on  212 Pb ( t  1/2 =10.6 h) are of interest for use as an  in vivo  generator of  α -particle emitting  212 Bi ( t  1/2 =60.6 min). Sterically stabilized liposomes were evaluated as carriers of  212 Pb/ 212 Bi radionuclides in the reported study.  212 Pb/ 212 Bi-containing vesicles were prepared by ionophore mediated loading of  212 Pb into preformed liposomes. The liposomal uptake of  212 Pb with or without various concentrations of lead carrier was investigated. The retention of  212 Pb and  212 Bi in liposomes incubated in serum was studied. Conditions were found yielding a high and rapid uptake of  212 Pb in liposomes. 90±2% of  212 Pb was incorporated after 30 min. The retention of radionuclides was high, 95% of  212 Pb and  212 Bi were retained in liposomes after incubating for 20 h at 37°C in serum. The results from the present work indicate that an effective retention of  212 Bi after the  β  - -decay of  212 Pb is achievable. This technology could be the basis of  α -emitting radiopharmaceuticals built upon  212 Pb.

radiochimica acta

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