Title: Cationic cholesterol derivative-based liposomes for enhanced cellular delivery of siRNA in serum
Abstract: Serum stability of cationic liposomes is a prerequisite for in vivo application of therapeutic genes. In this study, we report an enhancement of the serum stability and delivery efficiency of siRNA via use of newly synthesized cationic lipid-containing liposomes. Two cholesterol derivatives, cholesteryloxypropan-1-amine (COPA) and cholesteryl-2-aminoethylcarbamate (CAEC) were synthesized. Cationic liposomes were composed of DOPE and COPA or CAEC. Lipofectamine 2000 and CAEC-containing liposomes showed significantly reduced cellular uptake of siRNA after delivery in serum-containing media as compared to serum-free media. In contrast, COPA-basedliposomes revealed enhanced cellular uptake of siRNA in the presence of serum. The oncogene survivin-specific siRNA delivered via COPA-based liposomes reduced the mRNA expression levels of the target gene in Hepa 1-6 cells. The cytotoxicity of COPA-based liposomes was comparable to that of Lipofectamine 2000. These results suggest that the newly synthesized cholesterol derivative COPA-based liposomes could be further developed as a serum-stable non-viral delivery system of siRNA.
Publication Year: 2007
Publication Date: 2007-04-01
Language: en
Type: article
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