Synthesis of Fluorine-18 Functionalized Nanoparticles for use as in vivo Molecular Imaging Agents

Abstract

Nanoparticles containing fluorine-18 were prepared from block copolymers made by ring-opening metathesis polymerization (ROMP). Using the fast initiating ruthenium metathesis catalyst (H_2IMes)(pyr)_2(Cl)_2RuCHPh, narrow polydispersity, amphiphilic block copolymers were prepared from a cinnamoyl-containing, hydrophobic norbornene monomer and a mesylate-terminated, PEG-containing hydrophilic norbornene monomer. Self-assembly into micelles and subsequent crosslinking of the micelle cores by light-activated dimerization of the cinnamoyl groups yielded stable nanoparticles. Incorporation of fluorine-18 was achieved by nucleophilic displacement of the mesylates with the radioactive fluoride ion with 31% incorporation of radioactivity. The resulting positron-emitting nanoparticles are to be used as in vivo molecular imaging agents in tumor imaging.

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