Department of Applied Chemistry, Graduate School of Engineering, Osaka Prefecture University, 1-1 Gakuen-cho, Naka-ku, Sakai, Osaka 599-8531, Japan.
Biomacromolecules. 2010 Apr 12;11(4):1036-42. doi: 10.1021/bm1000108.
To improve the stability of a head-tail type polycation (PAMAM dendron-PLL), which is composed of a polyamidoamine (PAMAM) dendron head and poly(l-lysine) (PLL) tail blocks, as a gene vector against serum proteins, the PEGylation of the PAMAM dendron head was examined using physicochemical and transfection experiments. The PEGylation of the PAMAM dendron-PLL polyplexes neutralized the zeta-potential, indicating that the PEG brushes surround the surface of the polyplexes. The PEGylated PAMAM dendron-PLL polyplexes had higher tolerance against incubation with serum proteins when compared with non-PEGylated PAMAM dendron-PLL polyplexes. In addition, the transfection efficiency of the PEGylated PAMAM dendron-PLL polyplexes increased with increasing incubation periods, leading to an increase in the amount of pDNA uptaked by HeLa cells. Furthermore, effective stabilization of the PAMAM dendron-PLL polyplexes through PEGylation of the PAMAM dendron block was confirmed by the transfection experiments after preincubation with serum proteins and the PEGylated PAMAM dendron-PLL polyplexes showed a comparable level of transfection efficiency with polyethyleneimine polyplexes.
为了提高由聚酰胺胺（PAMAM）树枝状大分子头和聚（L-赖氨酸）（PLL）尾块组成的头-尾型聚阳离子（PAMAM 树枝状大分子-PLL）作为抗血清蛋白基因载体的稳定性，通过物理化学和转染实验研究了 PAMAM 树枝状大分子头的聚乙二醇化。PAMAM 树枝状大分子-PLL 超分子聚合物的聚乙二醇化使 Zeta 电位中和，表明 PEG 刷围绕超分子聚合物的表面。与非聚乙二醇化的 PAMAM 树枝状大分子-PLL 超分子聚合物相比，聚乙二醇化的 PAMAM 树枝状大分子-PLL 超分子聚合物对与血清蛋白孵育具有更高的耐受性。此外，随着孵育时间的增加，聚乙二醇化的 PAMAM 树枝状大分子-PLL 超分子聚合物的转染效率增加，导致 HeLa 细胞摄取的 pDNA 量增加。此外，通过 PAMAM 树枝状大分子块的聚乙二醇化对 PAMAM 树枝状大分子-PLL 超分子聚合物进行有效稳定化，通过与血清蛋白预孵育后的转染实验得到证实，并且聚乙二醇化的 PAMAM 树枝状大分子-PLL 超分子聚合物与聚乙烯亚胺超分子聚合物具有相当的转染效率。
