Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
5818779 | International Journal of Pharmaceutics | 2015 | 7 Pages |
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 25Â 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 (25Â kDa), therefore is an attractive candidate for further in vivo evaluation.
Graphical abstractIn this study, a reduction-sensitive cross-linked polyethylenimine derivative PEI-SS-OA was synthesized and evaluated for oligonucleotide delivery. PEI-SS-OA possesses both higher oligonucleotide delivery efficiency and lower cytotoxicity than PEI (25Â kDa), therefore is an attractive candidate for further in vivo evaluation.Download high-res image (176KB)Download full-size image