Alkane-modified short polyethyleneimine for siRNA delivery.
Alkane-modified short polyethyleneimine for siRNA delivery.
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DOI：
10.1016/j.jconrel.2011.11.030
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发表时间：
2012-06-10
期刊：
影响因子：
--
通讯作者：
Anderson DG
中科院分区：
文献类型：
--
作者：
Schroeder A;Dahlman JE;Sahay G;Love KT;Jiang S;Eltoukhy AA;Levins CG;Wang Y;Anderson DG
RNA interference (RNAi) is a highly specific gene-silencing mechanism triggered by small interfering RNA (siRNA). Effective intracellular delivery requires the development of potent siRNA carriers. Here, we describe the synthesis and screening of a series of siRNA delivery materials. Short polyethyleneimine (PEI, Mw 600) was selected as a cationic backbone to which lipid tails were conjugated at various levels of saturation. In solution these polymer–lipid hybrids self-assemble to form nanoparticles capable of complexing siRNA. The complexes silence genes specifically and with low cytotoxicity. The efficiency of gene knockdown increased as the number of lipid tails conjugated to the PEI backbone increased. This is explained by reducing the binding affinity between the siRNA strands to the complex, thereby enabling siRNA release after cellular internalization. These results highlight the importance of complexation strength when designing siRNA delivery materials.
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