Lee Kyung-Man, Lee Yong-Bok, Oh In-Joon
College of Pharmacy and Research Institute of Drug Development, Chonnam National University, Gwangju 500-757, Korea.
J Nanosci Nanotechnol. 2011 Aug;11(8):7078-81. doi: 10.1166/jnn.2011.4863.
Polyethylenimine (PEI) has been shown to be an efficient nonviral delivery vector. To improve its specificity and reduce its cytotoxicity, PEI should be modified. Transferrin (Tf) is a cell-binding ligand and Tf-receptors are expressed in malignant cells. Modification of cationic polymer by polyethylene glycol (PEG) can reduce the protein interaction and cell cytotoxicity of delivery vectors. We have synthesized PEG-Tf-PEI conjugate as an efficient and safe carrier of plasmid DNA (pDNA). Nanocomplexes of conjugates with pDNA were characterized by measuring the particle size and the surface charge. Transfection efficiency of nanocomplexes in Jurkat cells was improved and cytotoxicity was decreased compared with those of PEI complex. This was due to a reduction in the membrane damaging effect via shielding of the positive charge on the nanocomplex surface by PEG.
聚乙烯亚胺（PEI）已被证明是一种有效的非病毒递送载体。为了提高其特异性并降低其细胞毒性，应对PEI进行修饰。转铁蛋白（Tf）是一种细胞结合配体，且Tf受体在恶性细胞中表达。用聚乙二醇（PEG）修饰阳离子聚合物可减少递送载体的蛋白质相互作用和细胞毒性。我们已合成了PEG-Tf-PEI偶联物作为质粒DNA（pDNA）的高效且安全的载体。通过测量粒径和表面电荷对偶联物与pDNA的纳米复合物进行了表征。与PEI复合物相比，纳米复合物在Jurkat细胞中的转染效率提高，细胞毒性降低。这是由于PEG屏蔽了纳米复合物表面的正电荷，从而降低了膜损伤效应。
