Fluorocarbon Modified Low-Molecular-Weight Polyethylenimine for siRNA Delivery

Mark E. Johnson; Judy Shon; Brian M. Guan; Joseph P. Patterson; Nathan J. Oldenhuis; Alexander C. Eldredge; Nathan C. Gianneschi; Zhibin Guan

doi:10.1021/acs.bioconjchem.6b00216

Fluorocarbon Modified Low-Molecular-Weight Polyethylenimine for siRNA Delivery

Mark E. Johnson, Judy Shon, Brian M. Guan, Joseph P. Patterson, Nathan J. Oldenhuis, Alexander C. Eldredge, Nathan C. Gianneschi, Zhibin Guan^*

^*Corresponding author for this work

Chemistry

Research output: Contribution to journal › Article › peer-review

34 Scopus citations

Abstract

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.

Original language	English (US)
Pages (from-to)	1784-1788
Number of pages	5
Journal	Bioconjugate Chemistry
Volume	27
Issue number	8
DOIs	https://doi.org/10.1021/acs.bioconjchem.6b00216
State	Published - Aug 17 2016

ASJC Scopus subject areas

Biotechnology
Bioengineering
Biomedical Engineering
Pharmacology
Pharmaceutical Science
Organic Chemistry

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10.1021/acs.bioconjchem.6b00216

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title = "Fluorocarbon Modified Low-Molecular-Weight Polyethylenimine for siRNA Delivery",

abstract = "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.",

author = "Johnson, {Mark E.} and Judy Shon and Guan, {Brian M.} and Patterson, {Joseph P.} and Oldenhuis, {Nathan J.} and Eldredge, {Alexander C.} and Gianneschi, {Nathan C.} and Zhibin Guan",

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T1 - Fluorocarbon Modified Low-Molecular-Weight Polyethylenimine for siRNA Delivery

AU - Johnson, Mark E.

AU - Shon, Judy

AU - Guan, Brian M.

AU - Patterson, Joseph P.

AU - Oldenhuis, Nathan J.

AU - Eldredge, Alexander C.

AU - Gianneschi, Nathan C.

AU - Guan, Zhibin

PY - 2016/8/17

Y1 - 2016/8/17

N2 - 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.

AB - 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.

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Fluorocarbon Modified Low-Molecular-Weight Polyethylenimine for siRNA Delivery

Abstract

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