Gene transfer efficacies of serum-resistant amino acids-based cationic lipids: Dependence on headgroup, lipoplex stability and cellular uptake
Gene transfer efficacies of serum-resistant amino acids-based cationic lipids: Dependence on headgroup, lipoplex stability and cellular uptake
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基于血清抗性氨基酸的阳离子脂质的基因转移功效：取决于头基、脂质复合物稳定性和细胞摄取
DOI：
10.1016/j.ijpharm.2011.01.051
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发表时间：
2011-04-15
影响因子：
5.8
通讯作者：
Gu, Zhongwei
中科院分区：
文献类型：
--
作者：
Li, Li;Song, Hongmei;Gu, Zhongwei
血清是高效阳离子脂质体介导基因转染的主要障碍。本文以赖氨酸化胆固醇（脂质1）、组氨酸化胆固醇（脂质2）和精氨酸化胆固醇（脂质3）3种碱性氨基酸基阳离子脂质为非病毒基因载体。研究了由脂质1-3形成的脂质体的理化性质，如大小、Zeta电位、稳定性和细胞摄取，以及有血清或无血清转染的效果。结果表明，脂质1和脂质3在脂质体稳定性和细胞摄取方面表现出良好的特性。有趣的是，脂质3基脂质体对基因转染表现出血清增强作用。脂质1和脂质3的转染效率显著高于脂质2。此外，它们在含血清培养基中表现出比对照1,2-二聚环氧氧基-3-（三甲基胺）丙烷（DOTAP）脂质体高10-20倍的效果。这些数据表明，头群的类型对基因转染有很强的影响。赖氨酸/精氨酸衍生物阳离子脂质是一种很有前途的非病毒基因载体。(C) 2011 Elsevier B.V.版权所有
Serum is a major obstacle to efficient cationic liposome-mediated gene transfection. In this paper, three alkaline amino acids based cationic lipids including lysinylated cholesterol (lipid 1), histidinylated cholesterol (lipid 2) and argininylated cholesterol (lipid 3) were used as non-viral gene vectors. The physicochemical properties such as size, Zeta potential, stability and cellular uptake of the lipoplexes formed from lipids 1-3 as well as the transfection efficacies with or without serum were investigated. The results demonstrated that lipid 1 and lipid 3 showed good properties in lipoplex stability and cellular uptake. Interestingly, lipid 3-based liposome showed serum-enhanced effect on the gene transfection. The transfection efficiency of lipid 1 and lipid 3 was remarkably higher than that of lipid 2. Moreover, they exhibited 10-20-fold more efficaciously than the control, 1,2-dioleoyloxy-3-(trimethylammonio)propane (DOTAP) liposome in serum-containing media. The data suggested the strong effect of the type of the headgroup on gene transfection. The lysine/arginine derivative cationic lipids could be promising nonviral vectors for gene delivery in vivo. (C) 2011 Elsevier B.V. All rights reserved.