基于FA-PEG-PEI的顺铂/TFPI-2联合递送纳米系统的构建与表征-UDP糖丨MOF丨金属有机框架丨聚集诱导发光丨荧光标记推荐西安齐岳生物

文献：Preparation and Characterization of Folate-Targeted Fe3O4 Nanoparticle Codelivering Cisplatin and TFPI-2 Plasmid DNA for Nasopharyngeal Carcinoma Therapy

作者：Juan Zhang, Huanhuan Weng, Xiangwan Miao, Quanming Li, Siqi Wang, Huifen Xie, Tao Liu, Minqiang Xie

文献链接：https://onlinelibrary.wiley.com/doi/full/10.1155/2017/2849801

摘要：

A novel folate (FA) receptor-targeted superparamagnetic Fe3O4 nanoparticles (SPIONs) codelivering cisplatin (CDDP) and tissue factor pathway inhibitor-2 (TFPI-2) plasmid DNA (pDNA) was constructed. The core shell nanocomposites (FA-PEG-PEI@SPION-CDDP-TFPI-2) were composed of superparamagnetic Fe3O4 core that binds CDDP and TFPI-2 shell that combines with folate-polyethylene glycol-polyethyleneimine (FA-PEG-PEI) via electrostatic interaction. The shell containing FA-PEG-PEI and TFPI-2 plasmid was synthesized through amidation reaction and electrostatic adsorption and the core containing SPION-CDDP was modified by aldehyde sodium alginate. Proton nuclear magnetic resonance and Fourier transform infrared spectra on FA-PEG-PEI polymers showed characteristic peaks of various metabolites in corresponding frequency. Transmission electron microscopy image of FA-PEG-PEI@SPION-CDDP-TFPI-2 nanoparticles demonstrated a near-monodisperse spherical morphology, while dynamic light scattering studies indicated an intensity-average diameter of 149.5 nm. Zeta potential was 14.89 ± 1.83 mv and the final concentration of loaded CDDP was 100 ug/ml. Gel electrophoresis data showed that the nanocomposite would protect TFPI-2 pDNA from being digested by DNases. Compared with CNE-2 cells, the good targetability and better gene transfection efficiency (57.9%) were detected by Prussian blue iron stain and fluorescence analysis in HNE-1 cells in vitro. The results suggested the potential application of FA-PEG-PEI@SPION-CDDP-TFPI-2 as a multifunctional anticancer nanomedicine on targeting therapy for FR positive NPC.

FA-PEG-PEI

构建了一种新型叶酸（FA）受体靶向的超顺磁性Fe3O4纳米粒子（SPION），其可共同递送顺铂（CDDP）和组织因子途径抑制剂-2（TFPI-2）质粒DNA（pDNA）。

核壳纳米复合材料(FA-PEG-PEI@SPION-CDDP-TFPI-2)由结合CDDP的超顺磁性Fe3O4核和通过静电相互作用与叶酸聚乙二醇聚乙烯亚胺（FA-PEG-PEI）结合的TFPI-2壳组成。通过酰胺化反应和静电吸附合成了含有FA-PEG-PEI和TFPI-2质粒的外壳，并用海藻酸钠醛修饰了含有SPION-CDDP的核心。

FA-PEG-PEI聚合物的质子核磁共振和傅里叶变换红外光谱显示了相应频率下各种代谢物的特征峰。

透射电子显微镜图像FA-PEG-PEI@SPION-CDDP-TFPI-2纳米粒子表现出近乎单分散的球形形态，而动态光散射研究表明其强度平均直径为149.5 nm.Zeta电位为14.89±1.83 mv，负载CDDP的最终浓度为100 凝胶电泳数据显示，纳米复合材料可以保护TFPI-2 pDNA免受DNA酶的消化。

与CNE-2细胞相比，普鲁士蓝铁染色和荧光分析在HNE-1细胞中检测到良好的靶向性和更好的基因转染效率（57.9%）。