Fluorocarbon Modified Low-Molecular-Weight Polyethylenimine for siRNA Delivery
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- 作者：Mark E. Johnson ; Judy Shon ; Brian M. Guan ; Joseph P. Patterson ; Nathan J. Oldenhuis ; Alexander C. Eldredge ; Nathan C. Gianneschi ; Zhibin Guan
- 刊名：Bioconjugate Chemistry
- 出版年：2016
- 出版时间：August 17, 2016
- 年：2016
- 卷：27
- 期：8
- 页码：1784-1788
- 全文大小：324K
- 年卷期：0
- ISSN：1520-4812
文摘
We report the synthesis and study of fluorocarbon (FC) modified polyethylenimine (PEI) for the purpose of siRNA delivery. Low-molecular-weight PEI (Mn = 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.