| 欧阳湖,宁玲,陈思维,贺冬秀,王肖,何健,谢伟全.核酸适配体修饰聚酰胺-胺负载5-氟尿嘧啶纳米给药体系的制备表征及体外抗肝癌作用.[J].中南医学科学杂志.,2021,(6):630-635. |
| 核酸适配体修饰聚酰胺-胺负载5-氟尿嘧啶纳米给药体系的制备表征及体外抗肝癌作用 |
| Fabrication and characterization of aptamer modified polyamide-amine loaded 5-fluorouracil drug delivery system for hepatocellular carcinoma therapy in vitro |
| 投稿时间：2021-03-02 修订日期：2021-05-18 |
| DOI：10.15972/j.cnki.43-1509/r.2021.06.003 |
| 中文关键词: 肝细胞癌 5-氟尿嘧啶 核酸适配体 聚酰胺-胺 给药体系 |
| 英文关键词:hepatocellular carcinoma 5-fluorouracil aptamer polyamide amine drug delivery system |
| 基金项目:湖南省自然科学基金面上项目(2019JJ40256)；湖南省教育厅创新平台开放基金项目(17K082)；南华大学船山学院大学生创新创业训练计划项目(2019CX002) 作者简介:欧阳湖,硕士研究生,研究方向为抗肿瘤药物传递系统,E-mail为695887426@qq.com。通信作者贺冬秀,博士,副教授,硕士研究生导师,研究方向为药物评估与药物合成设计,E-mail为1025165380@qq.com。 |
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| 中文摘要: |
| 目的研究核酸适配体(ZY1)修饰聚酰胺-胺(PAMAM)负载5-氟尿嘧啶-1-基乙酸(FUA)纳米给药体系(ZY1-PAMAM-FUA)的制备表征及其体外抗肝癌作用。方法将FUA、聚乙二醇(PEG)与PAMAM通过酰胺反应键合,然后将ZY1通过静电吸附与PEG-PAMAM-FUA缀合得到ZY1-PAMAM-FUA纳米给药体系。核磁共振氢谱仪(1H-NMR)和傅里叶红外光谱仪(FT-IR)鉴定ZY1-PAMAM-FUA的化学结构,动态光散射技术(DLS)表征其粒径分布以及稳定性,紫外分光光度法检测其载药量和体外释药性能,流式细胞仪和荧光显微镜考察SMMC-7221肝癌细胞对Cy5标记的纳米给药体系的摄取能力；MTT法检测纳米给药体系对SMCC-7721肝癌细胞增殖活性的影响。结果ZY1-PAMAM-FUA粒径分布均匀,粒径为102.3 nm,其载药量为8.70%±0.43%,并具有良好的缓释性能。与PAMAM-FUA比较,ZY1-PAMAM-FUA可以更高效地靶向SMCC-7721细胞。ZY1-PAMAM-FUA具有良好的生物相容性且对SMCC-7721细胞具有良好的抗细胞增殖作用。结论ZY1-PAMAM-FUA制备方法简单稳定,具有良好的生物相容性,可以高效地将药物靶向SMCC-7721细胞发挥抗肝癌细胞增殖的作用。 |
| 英文摘要: |
| To study fabrication and characterization of the aptamer(ZY1) modified polyamide-amine (PAMAM) loaded 5-fluorouracil-1-glycolic acid (FUA) drug elivery system (ZY1-PAMAM-FUA) for hepatocellular carcinoma therapy in vitro. MethodsFUA, PEG and PAMAM are bonded through amide reaction, and then ZY1 is conjugated with PEG-PAMAM-FUA through electrostatic adsorption to obtain ZY1-PAMAM-FUA drug delivery system. The structure of ZY1-PAMAM-FUA was identified by nuclear magnetic resonance spectrometer (1H-NMR) and fourier infrared spectrometer (FT-IR). The particle size distribution and the stability of ZY1-PAMAM-FUA were characterized by dynamic light scattering (DLS). The drug loading and cumulation drug release in vitro were detected by ultraviolet spectrophotometry (UV). The cellular uptake ability of Cy5-labeled ZY1-PAMAM-FUA drug delivery system on SMMC-7221 cells were investigated by Flow cytometry and Fluorescence microscope. The effect of ZY1-PAMAM-FUA drug delivery system on the proliferation of SMCC-7721 cells was detected by MTT. ResultsZY1-PAMAM-FUA drug delivery system has uniform particle size distribution and good sustained release performance with particle size of 102.3 nm and drug loading of 8.70%±0.43%. Compared with PAMAM-FUA, ZY1-PAMAM-FUA can target SMCC-7721 cells more efficiently. ZY1-PAMAM-FUA has splendid biocompatibility and excellent anti-proliferation effect on SMCC-7721 cells.ConclusionsThe preparation method of ZY1-PAMAM-FUA is simple, and the ZY1-PAMAM-FUA drug delivery system has splendid stability and biocompatibility. It can effectively deliver drugs to SMCC-7721 cells to inhibit the proliferation of hepatocellular carcinoma cells. |
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