Department of Bioengineering and Institute for Bioengineering and Biopharmaceutical Research, Hanyang University, Seoul 133-791, Republic of Korea.
Carbohydr Polym. 2013 Jan 30;92(1):57-62. doi: 10.1016/j.carbpol.2012.08.116. Epub 2012 Sep 8.
Chitosan-based nanoparticles have been widely used as a carrier for gene delivery due to their low toxicity and the positively charged amino groups in chitosan. In this study, we hypothesized that introduction of nonaarginine to chitosan could improve its ability to form a complex with siRNA, as well as enhance the cellular uptake and transfection efficiency of chitosan-based nanoparticles. To this end, a peptide with nine repeating arginine residues was chemically coupled to the chitosan backbone, and various characteristics of nonaarginine-chitosan/siRNA nanoparticles were investigated. The mean diameter and zeta potential of the nonaarginine-chitosan/siRNA nanoparticles were dependent on the amount of nonaarginine conjugated to chitosan. Nonaarginine-modified chitosan/siRNA nanoparticles demonstrated enhanced cellular association and transfection efficiency in vitro, while maintaining a low level of cytotoxicity. In conclusion, nonaarginine-modified chitosan should be considered a potential carrier for various gene delivery applications.
壳聚糖基纳米粒子由于其低毒性和壳聚糖中带正电荷的氨基，已被广泛用作基因传递的载体。在这项研究中，我们假设向壳聚糖中引入九聚精氨酸可以提高其与 siRNA 形成复合物的能力，并增强壳聚糖基纳米粒子的细胞摄取和转染效率。为此，我们通过化学方法将具有九个重复精氨酸残基的肽连接到壳聚糖主链上，并研究了九聚精氨酸-壳聚糖/siRNA 纳米粒子的各种特性。九聚精氨酸-壳聚糖/siRNA 纳米粒子的平均直径和 zeta 电位取决于与壳聚糖结合的九聚精氨酸的量。九聚精氨酸修饰的壳聚糖/siRNA 纳米粒子在体外表现出增强的细胞结合和转染效率，同时保持低细胞毒性。总之，九聚精氨酸修饰的壳聚糖应该被认为是各种基因传递应用的潜在载体。
