Synthesis of Poly(propylene glycol)-block-Polyethylenimine Triblock Copolymers for the Delivery of Nucleic Acids

被引:10
作者
Brissault, Blandine [2 ]
Leborgne, Christian [1 ]
Scherman, Daniel [3 ]
Guis, Christine [4 ]
Kichler, Antoine [1 ,3 ]
机构
[1] Genethon, F-91002 Evry, France
[2] Equipe Syst Polymeres Complexes, Inst Chim & Mat Paris Est, UMR 7182, F-94320 Thiais, France
[3] Univ Paris 05, CNRS, INSERM, UMR 8151,U1022, Paris, France
[4] Univ Evry, Lab Anal & Modelisat Biol & Environn, UMR 8587, CNRS CEA UEVE, F-91025 Evry, France
关键词
amphiphiles; block copolymers; drug delivery systems; self-assembly; small interfering RNA; LINEAR POLYETHYLENIMINE; RNA INTERFERENCE; SIRNA DELIVERY; IN-VIVO; MAMMALIAN-CELLS; GENE DELIVERY; BEHAVIOR; DERIVATIVES; VITRO;
D O I
10.1002/mabi.201000404
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
LPEIs, which are efficient DNA transfection agents, were found to be far less effective for the delivery of siRNAs. Here, two amphiphilic triblock copolymers LPEI(50)-b-PPG(36)-b-LPEI(50) (2) and LPEI(14)-b-PPG(68)-b-LPEI(14) (4) have been synthesized. The transfection assays showed that compound 2 was efficient for DNA transfection whilst it was almost inactive for siRNA delivery. In contrast, polymer 4 was inefficient for DNA transfection while it showed capabilities for siRNA delivery. Taken together, our results indicate that the properties required for DNA and siRNA delivery are different. Moreover, we show that introduction of a hydrophobic segment that allows self-assembly confers siRNA delivery capacities.
引用
收藏
页码:652 / 661
页数:10
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