Spermine grafted galactosylated chitosan for improved nanoparticle mediated gene delivery
Spermine grafted galactosylated chitosan for improved nanoparticle mediated gene delivery
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DOI：
10.1016/j.ijpharm.2011.02.067
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发表时间：
2011-05-30
影响因子：
5.8
通讯作者：
Sharma, Chandra P.
中科院分区：
文献类型：
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作者：
Alex, Susan M.;Rekha, M. R.;Sharma, Chandra P.
尽管具有许多有益的特征，但壳聚糖具有差的水溶性和转染能力，这影响其基因递送功效。当某些化学改性并入壳聚糖母体骨架中时，这两个特征得到改善。这里采用这种策略，通过将半乳糖和精胺偶联到壳聚糖主链中。用FTIR和H-1 NMR确定共轭，并通过TEM和AFM技术评估纳米颗粒的形态。颗粒大小、zeta电位、缓冲能力和DNA结合能力给出了令人鼓舞的结果，增强了溶解性和稳定性。在体外研究中，GCSM在HepG 2细胞系中显示出低细胞毒性和改善的转染。我们还通过细胞摄取抑制剂处理确定了受体介导的内化对纳米颗粒细胞摄取的偏好。结果表明，半乳糖基化壳聚糖-g-精胺是一种很有前途的纳米粒介导基因传递的壳聚糖衍生物。(C)2011 Elsevier B. V.保留所有权利。
Despite multitude of beneficial features, chitosan has poor water solubility and transfection ability which affect its gene delivery efficacy. The two features are improved when certain chemical modifications are incorporated into the chitosan parent backbone. This strategy is adopted here, by coupling galactose and spermine into the chitosan backbone. The conjugation was determined with FTIR and H-1 NMR and nanoparticle morphology was assessed by TEM and AFM techniques. Particle size, zeta potential, buffering capacity and DNA binding ability gave encouraging result of enhanced solubility and stability. In vitro studies of GCSM in HepG2 cell lines displayed low cytotoxicity and improved transfection. We also identified the preference of receptor mediated internalization for nanoparticles cellular uptake by treating with cellular uptake inhibitors. The results evidently led us to comprehend that galactosylated chitosan-g-spermine could be considered as a promising chitosan derivative for conducting nanoparticle mediated gene delivery. (C) 2011 Elsevier B.V. All rights reserved.