A novel reduction-sensitive modified polyethylenimine oligonucleotide vector

作者：Yang, Shuang; Lee, Robert J.; Yang, Xuewei; Zheng, Bin; Xie, Jing; Meng, Lingjun; Liu, Yan; Teng, Lesheng^*

来源：International Journal of Pharmaceutics, 2015, 484(1-2): 44-50.

DOI：10.1016/j.ijpharm.2015.02.036

• Polyethylenimine
• Reduction-sensitive
• Disulfide
• Oligonucleotide delivery

A reduction-sensitive cross-linked polyethylenimine derivative PEI-SS-OA was synthesized and evaluated for oligonucleotide delivery. PEI-SS-OA was shown to condense LOR-2501, an oligonucleotide targeting ribonucleotide reductase R1 subunit (RRM1), into positively charged complexes. The reductive degradation of the PEI-SS-OA induced by dithiothreitol was confirmed by a gel retardation assay. In vitro experiments revealed that the reduction-sensitive PEI-SS-OA was less cytotoxic and more effective in oligonucleotide delivery than the control 25 kDa PEI. This study demonstrates that a reducibly degradable cationic polymer PEI-SS-OA possesses both higher oligonucleotide delivery efficiency and lower cytotoxicity than PEI (25 kDa), therefore is an attractive candidate for further in vivo evaluation.

• 出版日期2015-4-30
• 单位吉林大学