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Quaternization enhances the transgene expression efficacy of aminoglycoside-derived polymers.

Abstract：

:The objective of the present study was to synthesize and investigate the transgene expression efficacy of quaternized derivatives of aminoglycoside polymers in different cancer cell lines. A series of glycidyltrimethylammonium chloride (GTMAC) derivatives of aminoglycoside polymers (GTMAC-AM polymers), containing varying degrees of quaternization (13-45%), were synthesized. The structures and properties of GTMAC-AM polymers were investigated using FT-IR and (1)H NMR spectroscopy. Physicochemical factors that influence transgene expression efficacy including DNA binding, hydrodynamic size, zeta potential and cytotoxicity, were determined. Formation of polymer-plasmid DNA complexes was also visualized using atomic force microscopy. GTMAC-AM polymers demonstrated higher transgene expression efficacies compared to their parent polymers, 25 kDa poly(ethyleneimine), as well as Lipofectamine-3000. Our results indicate that quaternization enhances the transgene expression efficacy and reduces the cytotoxicity of aminoglycoside-derived polymers, making it an attractive strategy for nucleic acid delivery with these new materials.

journal_name

Int J Pharm

journal_title

International journal of pharmaceutics

authors

Miryala B,Feng Y,Omer A,Potta T,Rege K

doi

10.1016/j.ijpharm.2015.04.026

subject

Has Abstract

pub_date

2015-07-15 00:00:00

pages

18-29

issue

1-2

eissn

0378-5173

issn

1873-3476

pii

S0378-5173(15)00334-8

journal_volume

489

pub_type

杂志文章

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