Fluorocarbon Modified Low-Molecular-Weight Polyethylenimine for siRNA Delivery

被引：41

作者：

Johnson, Mark E. ^{[1
]}

Shon, Judy ^{[1
]}

Guan, Brian M. ^{[1
]}

Patterson, Joseph P. ^{[2
]}

Oldenhuis, Nathan J. ^{[1
]}

Eldredge, Alexander C. ^{[1
]}

Gianneschi, Nathan C. ^{[2
]}

Guan, Zhibin ^{[1
]}

机构：

[1] Univ Calif Irvine, Dept Chem, Irvine, CA 92697 USA

[2] Univ Calif San Diego, Dept Chem & Biochem, La Jolla, CA 92093 USA

来源：

BIOCONJUGATE CHEMISTRY | 2016年 / 27卷 / 08期

关键词：

LIPID-LIKE MATERIALS; RNAI THERAPEUTICS; CATIONIC LIPIDS; NANOPARTICLES; DESIGN; LIPOSOMES; POLYMERS; LIBRARY; POTENT; DNA;

D O I：

10.1021/acs.bioconjchem.6b00216

中图分类号：

Q5 [生物化学];

学科分类号：

071010 ; 081704 ;

摘要：

We report the synthesis and study of fluorocarbon (FC) modified polyethylenimine (PEI) for the purpose of siRNA delivery. Low-molecular-weight PEI (M-n = 600) was functionalized with fluorocarbon epoxides of varying length. All FC-modified samples with greater than 2.0 equiv of FC epoxide per PEI induced potent gene silencing in vitro. Compared to hydrocarbon (HC) analogues, the FC vectors showed greater general silencing efficacy, higher cell uptake, and reduced association with serum components. Collectively, the data suggest that modification of polyamines with FCs is a promising approach for the discovery of novel vectors for siRNA delivery.

引用

页码：1784 / 1788

页数：5

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