Huang Yongzhuo, Chen Jinliang, Chen Xiaojin, Gao Jianqing, Liang Wenquan
College of Pharmaceutical Sciences, Zhejiang University, 388 Yuhangtang Road, Hangzhou, P.R. China.
J Mater Sci Mater Med. 2008 Feb;19(2):607-14. doi: 10.1007/s10856-007-3193-4. Epub 2007 Jul 10.
Polyethylene glycol (PEG) modified cationic niosomes were used to improve the stability and cellular delivery of oligonucleotides (OND). PEGylated cationic niosomes, composed of DC-Chol, PEG2000-DSPE and the non-ionic surfactant-Span, offer some advantages as gene carriers. Complexes of PEGylated cationic niosomes and OND showed a neutral zeta potential with particle size about 300 nm. PEG-modification significantly decreased the binding of serum protein and prevented particle aggregation in serum. The loaded nuclear acid drug exhibited increased resistance to serum nuclease. Compared with cationic niosomes, the PEGylated niosomes showed a higher efficiency of OND cellular uptake in serum. Therefore, in terms of their stable physiochemical properties in storage and physiological environment, as well as low-cost and widely available materials, PEGylated cationic niosomes are promising drug delivery systems for improved OND potency in vivo.
聚乙二醇（PEG）修饰的阳离子脂质体被用于提高寡核苷酸（OND）的稳定性和细胞递送能力。由二油酰基磷脂酰胆碱（DC-Chol）、聚乙二醇2000-二硬脂酰基磷脂酰乙醇胺（PEG2000-DSPE）和非离子表面活性剂司盘组成的聚乙二醇化阳离子脂质体作为基因载体具有一些优势。聚乙二醇化阳离子脂质体与OND的复合物呈现中性ζ电位，粒径约为300 nm。PEG修饰显著降低了血清蛋白的结合，并防止了血清中的颗粒聚集。负载的核酸药物对血清核酸酶的抗性增强。与阳离子脂质体相比，聚乙二醇化脂质体在血清中对OND的细胞摄取效率更高。因此，就其在储存和生理环境中的稳定理化性质以及低成本和广泛可用的材料而言，聚乙二醇化阳离子脂质体是有望提高体内OND效力的药物递送系统。
