Phenylboronic acid-conjugated cationic methylcellulose for hepatocellular carcinoma-targeted drug/gene co-delivery systems

摘要

Phenylboronic acid-conjugated cationic methylcellulose (MCPEI-PBA) was synthesized and characterized for hepatocellular carcinoma-targeted drug/gene co-delivery systems. MCPEI-PBA was obtained by reductive amination of polyethylenimine 2k to oxidized methylcellulose and conjugation of PBA. MCPEI-PBA could form nano-aggregates via B-N coordinate bonding and hydrophobic interaction and also form positively charged and nano-sized polyplexes. Cytotoxicity of MCPEI-PBA was low and MCPEI-PBA showed higher transfection efficiency than PEI25k in hepatocellular carcinoma. Galactose pretreatment experiment suggested its specific interaction with asialoglycoprotein receptors. MCPEI-PBA could encapsulate doxorubicin (Dox) efficiently. Finally, MCPEI-PBA/Dox/pJDK-apoptin complexes showed high anticancer activity due to the combinatorial effect of Dox and expressed apoptin. (C) 2019 The Korean Society of Industrial and Engineering Chemistry. Published by Elsevier B.V. All rights reserved.