Polymeric nanoparticles for dual-targeted theranostic gene delivery to hepatocellular carcinoma.

Vaughan, Hannah J; Zamboni, Camila G; Hassan, Laboni F; Radant, Nicholas P; Jacob, Desmond; Mease, Ronnie C; Minn, Il; Tzeng, Stephany Y et al. · Sci Adv · 2022

basic_science · Level V

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Abstract

Hepatocellular carcinoma (HCC) develops predominantly in the inflammatory environment of a cirrhotic liver caused by hepatitis, toxin exposure, or chronic liver disease. A targeted therapeutic approach is required to enable cancer killing without causing toxicity and liver failure. Poly(beta-amino-ester) (PBAE) nanoparticles (NPs) were used to deliver a completely CpG-free plasmid harboring mutant herpes simplex virus type 1 sr39 thymidine kinase (sr39) DNA to human HCC cells. Transfection with sr39 enables cancer cell killing with the prodrug ganciclovir and accumulation of 9-(4-<sup>18</sup>F-fluoro-3-hydroxymethylbutyl)guanine (<sup>18</sup>F-FHBG) for in vivo imaging. Targeting was achieved using a CpG-free human alpha fetoprotein (AFP) promoter (CpGf-AFP-sr39). Expression was restricted to AFP-producing HCC cells, enabling selective transfection of orthotopic HCC xenografts. CpGf-AFP-sr39 NP treatment resulted in 62% reduced tumor size, and therapeutic gene expression was detectable by positron emission tomography (PET). This systemic nanomedicine achieved tumor-specific delivery, therapy, and imaging, representing a promising platform for targeted treatment of HCC.

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