Liu Xin-Yi, Ho Wen-Yueh, Hung Wei Jing, Shau Min-Da
Department of Graduate Institute of Pharmaceutical Science, Chia-Nan University of Pharmacy and Science, Tainan 71710, Taiwan.
Biomaterials. 2009 Dec;30(34):6665-73. doi: 10.1016/j.biomaterials.2009.08.052. Epub 2009 Sep 22.
To improve the transfection efficiency of polycations with DNA, we synthesized poly(ester-co-urethane)(PEU-g-PEI800) with short chain PEI800 in the side chain, and poly(ester-co-urethane)(PEU) without short chain PEI800. Both PEU-g-PEI800 and PEU, readily self-assembled with plasmid DNA (pCMV-betagal) in a HEPES buffer, were characterized by dynamic light scattering and zeta-potential. The results reveal that PEU-g-PEI800 and PEU were able to self-assemble particles with DNA and yield nano-sized complexes (<200nm) with positive charge at N/P ratios of 20/1 and 120/1, respectively. The degradation studies indicate that the half-life of PEU-g-PEI800 and PEU in the HEPES buffer were 14 and 35h at pH 7.4, respectively. Titration studies were performed to determine the buffering capacities of the polymers. The COS-7 cell viabilities in the presence of PEU-g-PEI800/DNA, PEU/DNA, and PEI25k/DNA were studied. In addition, The PEU-g-PEI800/DNA complexes were able to transfect COS-7 cells in vitro with a high efficiency comparable to a well-known gene carrier PEI25k. The results indicate that PEU-g-PEI800 is an attractive cationic poly (ester-co-urethane) for gene delivery and an interesting candidate for further study.
为提高聚阳离子与DNA的转染效率，我们合成了侧链带有短链PEI800的聚（酯-共-聚氨酯）（PEU-g-PEI800）以及没有短链PEI800的聚（酯-共-聚氨酯）（PEU）。PEU-g-PEI800和PEU在HEPES缓冲液中均能与质粒DNA（pCMV-β半乳糖苷酶）轻松自组装，通过动态光散射和zeta电位对其进行了表征。结果表明，PEU-g-PEI800和PEU能够与DNA自组装形成颗粒，并分别在N/P比为20/1和120/1时产生带正电荷的纳米级复合物（<200nm）。降解研究表明，在pH 7.4时，PEU-g-PEI800和PEU在HEPES缓冲液中的半衰期分别为14小时和35小时。进行了滴定研究以确定聚合物的缓冲能力。研究了在存在PEU-g-PEI800/DNA、PEU/DNA和PEI25k/DNA的情况下COS-7细胞的活力。此外，PEU-g-PEI800/DNA复合物能够在体外高效转染COS-7细胞，其效率与著名的基因载体PEI25k相当。结果表明，PEU-g-PEI800是一种有吸引力的用于基因递送的阳离子聚（酯-共-聚氨酯），是进一步研究的有趣候选物。
