Bioreducible polyspermine as less toxic and efficient gene carrier

Abstract

Bioreducible polymers have attracted intense attention as a gene carrier due to their low cell toxicity compared to other polymer‐based gene delivery counterparts. We have synthesized low‐molecular‐weight spermine‐originated bioreducible polyspermines (BPSs) to serve as a plasmid DNA (pDNA) carrier complex with low cytotoxicity and high transfection efficiency. Spermine is biogenic and ubiquitous and is of benefit to nucleic acid delivery in many respects. We found that the BPSs formed nano‐sized, positively charged complexes with pDNA. In addition, they showed a high buffering capacity from the polyamine‐based proton sponge effect which facilitates endosomal escape. With degradable characteristics in thiol‐rich (intracellular) environments, BPSs exhibited significantly improved cell viability and suitable transfection efficiency across several cell lines in comparison to linear and branched polyethylenimine, the current gold standards of non‐viral gene carriers. BPSs appear to be promising polymers for use as effective pDNA carriers. Copyright © 2014 John Wiley & Sons, Ltd.

Combinatorial gene construct and non-viral delivery for anti-obesity in diet-induced obese mice

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Advances in redox-responsive drug delivery systems of tumor microenvironment

“…Therefore, existing delivery systems that are based on the mercapto polymerization are very rare. There was a study utilizing mercapto polymerization to modify spermine with thiolate, and a gene carrier named bioreducible polyspermine (BPS) with linear structures was successfully synthesized [ 29 ]. Different BPS with various molecular weight (27.5 kDa, 15.7 kDa and 6.1 kDa) were analyzed in this study.…”

Dendritic Cell-Targeted pH-Responsive Extracellular Vesicles for Anticancer Vaccination

“…In particular, protonation of amines in pH-sensitive molecules results in buffering inside endosomes after they are endocytosed followed by osmotic swelling and endosomolysis. The “proton sponge” effect leads to the endosomal escape of drug delivery agents from lysosomal degradation together with the release of therapeutic payloads from the delivery devices [ 29 , 30 , 31 , 32 ]. Moreover, to promote the selective interaction between a targeted cell and a delivery tool, the ligand–receptor system can be exploited further.…”