Aptamer-Functionalized Drug Nanocarrier Improves Hepatocellular Carcinoma toward Normal by Targeting Neoplastic Hepatocytes.

Site-specific delivery of chemotherapeutics specifically to neoplastic hepatocytes without affecting normal hepatocytes should be a focus for potential therapeutic management of hepatocellular carcinoma (HCC). The aptamer TLS 9a with phosphorothioate backbone modifications (L5) has not been explored so far for preferential delivery of therapeutics in neoplastic hepatocytes to induce apoptosis. Thus, the objective of the present investigation was to compare the therapeutic potential of L5-functionalized drug nanocarrier (PTX-NPL5) with those of the other experimental drug nanocarriers functionalized by previously reported HCC cell-targeting aptamers and non-aptamer ligands, such as galactosamine and apotransferrin.

A Comparative Investigation of the Ability of Various Aptamer-Functionalized Drug Nanocarriers to Induce Selective Apoptosis in Neoplastic Hepatocytes: In Vitro and In Vivo Outcome.

Aptamers offer a significant promise to target various cancers including hepatocellular carcinoma (HCC), for their high affinity and ability to reach the target site(s), non-immunogenicity, and low cost. The targeting ability to neoplastic hepatocytes by the aptamer, TLS 9a with phosphorothioate backbone modification (designated as L5), has not been explored yet. Hence, we investigated the comparative potential of L5 with some other previously reported liver cancer cell-specific aptamers, conjugated on the surface of drug-nanocarriers.