Investigation of a tellurium-packed column for isolation of astatine-211 from irradiated bismuth targets and demonstration of a semi-automated system

Astatine-211 is an attractive radionuclide for use in targeted alpha therapy of blood-borne diseases and micrometastatic diseases. Efficient isolation methods that can be adapted to robust automated ²¹¹At isolation systems are of high interest for improving the availability of ²¹¹At. Based on the early studies of Bochvarova and co-workers involving isolation of ²¹¹At from irradiated thorium targets, we developed a method for ²¹¹At isolation from bismuth targets using tellurium-packed columns. Dissolution of irradiated bismuth targets is accomplished using HNO₃; however, ²¹¹At is not captured on the Te column material in this matrix. Our method involves slow addition of aqueous NH₂OH·HCl to the Bi target dissolved in HNO₃ to convert to a HCl matrix. The amount of NH₂OH·HCl was optimized because (1) the quantity of NH₂OH·HCl used appears to affect the radiolabeling yield of phenethyl-closo-decaborate(2-) (B10)-conjugated antibodies and (2) reducing the volume of NH₂OH·HCl solution can effectively shorten the overall isolation time. A proof-of-concept semi-automated process has been demonstrated using targets containing ~0.96 GBq (~26 mCi) of ²¹¹At. High isolation yields (88-95%) were obtained. Radiochemical purity of the isolated ²¹¹At was assessed by radio-HPLC. Concentrations of Bi and Te contaminants in the ²¹¹At and the astatinated antibodies were evaluated using ICP-MS.