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本研究通过体外评价比较了不同阳离子脂材(DC-Chol和DOTAP),不同比例PEG修饰的阳离子脂质体对siRNA细胞转染效果的影响。体外细胞转染实验结果表明,DOTAP转染能力强于DC-Chol;2%摩尔比例的PEG可增强细胞内siRNA的摄取。以DOTAP为阳离子脂材的PEG修饰的脂质体与siRNA形成复合物粒径在100nm左右,并能减少脂质体与血清中蛋白的相互作用,从而可能保护siRNA并延长体内循环时间。与阳性转染试剂lipofectamine 2000相比,该脂质体能有效输送siRNA进入细胞,并从溶酶体中逃逸。该脂质体可进行进一步的修饰,有可能应用于siRNA跨膜转运,并最终用于临床疾病的治疗。
In this study, the effects of cationic liposomes with different cationic lipids (DC-Chol and DOTAP) and different proportions of PEG-modified cationic liposomes on the transfection efficiency of siRNA cells were compared in vitro. In vitro cell transfection experiments showed that DOTAP transfection ability is stronger than DC-Chol; 2% molar ratio of PEG can enhance intracellular siRNA uptake. The PEG-modified liposomes with DOTAP as cationic lipids form a complex particle size of about 100 nm with siRNA, and can reduce the interaction of liposomes with serum proteins, thereby possibly protecting the siRNA and prolonging the circulation time in the body. Compared with the lipofectamine 2000, a positive transfection reagent, this liposome effectively transports siRNA into cells and escapes from lysosomes. This liposome can be further modified, potentially for translocation of siRNAs and ultimately for the treatment of clinical conditions.