Department of Chemical & Materials Engineering, Faculty of Engineering, University of Alberta, Edmonton, AB, Canada.
Macromol Biosci. 2011 May 12;11(5):662-72. doi: 10.1002/mabi.201000402. Epub 2011 Feb 14.
Characterization of a polymer library engineered to enhance their ability to protect and deliver their nucleotide cargo to the cells is reported. The ζ-potential continuously increased with higher polymer:siRNA weight ratio, and the ζ-potential of lipid-modified polymers:siRNA complexes were higher than PEI2 at all ratios. At polymer:siRNA ratio of 1:1, all lipid-substituted polymers showed complete protection against degradation. Lipid-modified polymers significantly increased the cellular uptake of siRNA complexes and down-regulation of GAPDH and P-gp (max. 66% and 67%, respectively). The results indicate that hydrophobic modification of low molecular PEI could render this otherwise ineffective polymer to a safe effective delivery system for intracellular siRNA delivery and protein silencing.
本文报道了一种聚合物文库的特性研究，该文库经过设计可增强其保护和将核苷酸货物递送到细胞的能力。ζ-电位随聚合物与 siRNA 的重量比的增加而持续增加，并且所有比例下，脂质修饰聚合物与 siRNA 的复合物的 ζ-电位均高于 PEI2。在聚合物与 siRNA 的比例为 1:1 时，所有脂质取代聚合物均完全防止了降解。脂质修饰聚合物显著增加了 siRNA 复合物的细胞摄取，并下调了 GAPDH 和 P-糖蛋白（分别最大 66%和 67%）。结果表明，低分子量 PEI 的疏水性修饰可使这种原本无效的聚合物成为一种安全有效的用于细胞内 siRNA 递药和蛋白沉默的输送系统。
