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利用叶酸(FA)活性酯与O-羧甲基壳聚糖(O-CMC)合成了具有一定肿瘤靶向性的FA偶联O-CMC(FA-O-CMC),用核磁共振(1H-NMR)对其结构进行了表征。采用离子交联法,以CaCl2为交联剂,制得了Survivin siRNA/FA-O-CMC纳米粒。扫描电镜(SEM)、激光粒度仪和紫外-可见光谱等分析结果表明,纳米粒分散均匀,当CaCl2∶FA-O-CMC和siR-NA∶FA-O-CMC质量比分别为1∶5和1∶400时,纳米粒粒径为(199.5±23.5)nm,Zeta电位为(-17.39±2.16)mV,包封率和载药量分别为(88.96±1.53)%和(38.25±1.33)%,体外释放实验中,72 h基因释放75%,具有良好缓释性能。

Folate conjugated O-carboxymethyl chitosan (FA-O-CMC) possessing tumor targeting was synthesized via FA-ester and O-CMC, and the structure was confirmed by 1H-NMR spectroscopy. Survivin siRNA encapsulated FA-O-CMC nanoparticles were prepared through a cross-linking approach with CaC12. The results of scanning electron microscope (SEM), laser particle size analysis and UV spectra show that the prepared particles are homogeneously dispersed with small particles size (199.5 ± 23.5 nm) and the Zeta potential is (-17.39 ± 2.16) mV when the mass ratios of CaCl2 and siRNA to FA-O-CMC is selected as 1:5 and 1:400. Up to (88.96 ± 1.53) % of the encapsulation efficiency and (38.25 ± 1.33) % of the yield have been achieved to the Survivin siRNA gene. In vitro release shows, 75 % of Survivin siRNA is released after 72 h, exlibiting good controlled release property.

参考文献

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