Institute of Chemical Biology and Pharmaceutical Chemistry, Zhejiang University, Hangzhou, China.
Biomaterials. 2011 Oct;32(29):7253-62. doi: 10.1016/j.biomaterials.2011.06.015. Epub 2011 Jun 28.
Target ligand folic acid (FA) and cell-penetrating peptide octaarginine (R8) were coupled with the gene vectors (PEI(600)-CyD, PC) composed of β-cyclodextrin (β-CyD) and low-molecular-weight polyethylenimine (PEI, Mw 600) to form nanovectors for highly efficient gene delivery to tumor cells. The resultant ternary nanocomplexes of FA-PC/R8-PC/pDNA produced excellent gene transfaction abilities in the folate receptor (FR)-positive tumor cells in vitro and in vivo. The FR-mediated endocytosis and the R8-mediated transmembrane functionality together contributed to the high transfection levels. This study provides a promising means to produce gene nanovectors for in vivo applications.
靶向配体叶酸（FA）和细胞穿透肽八聚精氨酸（R8）与基因载体（PEI(600)-CyD、PC）偶联，该基因载体由β-环糊精（β-CyD）和低分子量聚乙烯亚胺（PEI，Mw 600）组成，形成纳米载体，可将基因高效递送至肿瘤细胞。所得的 FA-PC/R8-PC/pDNA 三元纳米复合物在体外和体内均表现出优异的转染能力，在叶酸受体（FR）阳性肿瘤细胞中。FR 介导的内吞作用和 R8 介导的跨膜功能共同促成了高转染水平。该研究为体内应用提供了一种有前途的基因纳米载体生产方法。
