Targeted melanoma radiotherapy using ultrasmall ¹⁷⁷Lu-labeled α-melanocyte stimulating hormone-functionalized core-shell silica nanoparticles.

ABSTRACT: Lutetium-177 (¹⁷⁷Lu) radiolabeled ultrasmall (~6 nm dia.) fluorescent core-shell silica nanoparticles (Cornell prime dots or C' dots) were developed for improving efficacy of targeted radiotherapy in melanoma models. PEGylated C' dots were surface engineered to display 10-15 alpha melanocyte stimulating hormone (αMSH) cyclic peptide analogs for targeting the melanocortin-1 receptor (MC1-R) over-expressed on melanoma tumor cells. The ¹⁷⁷Lu-DOTA-αMSH-PEG-C' dot product was radiochemically stable, biologically active, and exhibited high affinity cellular binding properties and internalization. Selective tumor uptake and favorable biodistribution properties were also demonstrated, in addition to bulk renal clearance, in syngeneic B16F10 and human M21 xenografted models. P

SUBMITTER: Zhang X 

PROVIDER: S-EPMC7171978 | biostudies-literature | 2020 May

REPOSITORIES: biostudies-literature