Synthesis and Properties of Targeted Radioisotope Carriers Based on Poly(Acrylic Acid) Nanogels

Radiation crosslinking was employed to obtain nanocarriers based on poly(acrylic acid)-PAA-for targeted delivery of radioactive isotopes. These nanocarriers are internally crosslinked hydrophilic macromolecules-nanogels-bearing carboxylic groups to facilitate functionalization. PAA nanogels were conjugated with an engineered bombesin-derivative-oligopeptide combined with 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetate chelating moiety, aimed to provide selective radioligand transport. 4-(4,6-Dimethoxy-1,3,5-triazin-2-yl)-4-methylmorpholinium (DMTMM) toluene-4-sulfonate was used as the coupling agent. After tests on a model amine-p-toluidine-both commercial and home-synthesized DOTA-bombesin were successfully coupled to the nanogels and the obtained products were characterized. The radiolabeling efficiency of nanocarriers with Lu-177, was chromatographically tested. The results provide a proof of concept for the synthesis of radiation-synthesized nanogel-based radioisotope nanocarriers for theranostic applications.

Automated summary

Radiation crosslinking was used to create nanocarriers based on poly(acrylic acid) for targeted delivery of radioactive isotopes. The internally crosslinked hydrophilic macromolecules-nanogels were conjugated with bombesin-derivative-oligopeptide and tetraazacyclododecane-1,4,7,10-tetraacetate for selective radioligand transport. The efficiency of radiolabeling nanocarriers with Lu-177 was chromatographically tested, showing promise for theranostic applications.