Synthesis and properties of a novel methoxy poly(ethylene glycol)-modified galactosylated chitosan derivative
Synthesis and properties of a novel methoxy poly(ethylene glycol)-modified galactosylated chitosan derivative
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DOI：
10.1007/s10856-008-3620-1
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发表时间：
2009-03
期刊：
影响因子：
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通讯作者：
Zhang Tao;Yuan Yu;D. Li;Rong Peng;Ying Li;Qing Jiang;Ping Dai;R. Gao
中科院分区：
文献类型：
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作者：
Zhang Tao;Yuan Yu;D. Li;Rong Peng;Ying Li;Qing Jiang;Ping Dai;R. Gao
壳聚糖及其衍生物是一种很有吸引力的非病毒载体。为了提高壳聚糖的靶细胞特异性和溶解性，合成了一种新型的半乳糖和甲氧基聚乙二醇（mPEG）修饰的壳聚糖衍生物，并对壳聚糖及其衍生物的结构变化进行了表征。与壳聚糖相比，新型壳聚糖衍生物的溶液粘度显著降低。半乳糖和mPEG对壳聚糖的取代度分别为0.09和0.30。含VRMFat质粒的mPEG化半乳糖基化壳聚糖（GaC）纳米粒的平均粒径为178 nm，zeta电位为+2.93 mV，表明其具有适合基因递送系统的性质。凝胶电泳证实质粒DNA完全被mPEG化的GaC纳米颗粒保留。并且，与对照壳聚糖相比，mPEG化GaC纳米颗粒对人胚肾（HEK 293）细胞的细胞毒性作用可以忽略不计。因此，预期mPEG化的GaC将具有作为靶向基因递送系统的进一步应用的潜力。
Chitosan and its derivatives are attractive non-viral vectors. To produce target-cell specificity and improve the solubility of chitosan, a novel chitosan derivative, modified with galactose and methoxy poly(ethylene glycol) (mPEG) was synthesized, and structure changes of chitosan and its derivatives were characterized. Compared to chitosan, the solution viscosity of the novel chitosan derivative drastically decreased. And, the degree of substitution (DS) of chitosan by galactose and mPEG were calculated as 0.09 and 0.30. The average diameter and zeta potential of mPEGylated galactosylated chitosan (GaC) nanoparticle containing VRMFat plasmid were 178 nm and +2.93 mV, suggesting suitable properties for gene delivery system. The gel electrophoresis confirmed that the plasmid DNA was remained completely by the mPEGylated GaC nanoparticle. And, the cytotoxic effect of mPEGylated GaC nanoparticles on human embryonic kidney (HEK 293) cells was negligible in comparison with that of control chitosans. Therefore, it is expected that the mPEGylated GaC will have the potential as a targeting gene delivery system for a further application.