Covalent core-radiolabeling of polymeric micelles with ¹²⁵I/²¹¹At for theranostic radiotherapy.

ABSTRACT: Astatine-211 (²¹¹At) is one of the most promising α-emitters for targeted alpha therapy, especially of cancer metastases. However, the lack of a stable isotope, frequent in vivo deastatination, and limited radiochemical knowledge makes it challenging to apply. Here, we report a new strategy for radiolabeling the lipophilic core of polymeric micelles (PMs) with covalently bound ²¹¹At. The PMs were radiolabeled via either an indirect synthon-based method or directly on the amphipathic block copolymer. The radiochemistry was optimized with iodine-125 (¹²⁵I) and then adapted for ²¹¹At, enabling the use of both elements as a potential theranostic pair. PMs that were core-radiolabeled with both ¹²⁵I or ²¹¹At were prepared a

SUBMITTER: Sporer E 

PROVIDER: S-EPMC9330252 | biostudies-literature | 2022

REPOSITORIES: biostudies-literature