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Design, synthesis, and characterization of glycyrrhetinic acid-mediated multifunctional liver-targeting polymeric carrier materials

机译:甘草酸介导的多功能肝靶向聚合物载体材料的设计,合成和表征

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摘要

The purpose of this study was to construct a glycyrrhetinic acid (GA)-mediated, breakable, intracellular, nanoscale drug-delivery carrier via amide and esterification reactions. The structures were identified by Fourier-transformed infrared (FTIR) and ~1H-nuclear magnetic resonance (~1H-NMR) spectrophotometry. The compatibility and safety of the carrier were evaluated using hemolysis and cytotoxicity tests. The GA-copolymer micelle was prepared using the solvent evaporation method. FTIR and ~1H-NMR detection demonstrated the successful construction of the polymer. No hemolysis occurred in any concentration of polymer within 3 h, and the hemolysis rate was less than 5%. 3-(4,5-dimethyl-thiazol-2-yl)-2,5-diphenyl-tetrazolium bromide (MTT) experimental results showed that the novel polymer reduced the cell survival rate and had significant cytotoxic effects. The blank nanoparticles were liquid with light blue opalescence. Transmission electron microscopy revealed that the empty micelles were uniform spheres, with an average size of 62 nm and a zeta potential of -13 mV. The novel GA-mediated polymeric carrier material developed here has the potential to effectively kill human SMMC-7721 cancer cells within 3 days when the dose is above 500 ug/mL.
机译:本研究的目的是通过酰胺和酯化反应来构建甘草酸(GA)介导的,可破坏,细胞内,纳米级药物输送载体。通过傅里叶转化的红外(FTIR)和〜1H核磁共振(〜1H-NMR)分光光度法鉴定该结构。使用溶血和细胞毒性试验评估载体的相容性和安全性。使用溶剂蒸发方法制备GA-共聚物胶束。 FTIR和〜1H-NMR检测证明了聚合物的成功构建。在3小时内的任何聚合物中没有发生溶血,溶血率小于5%。 3-(4,5-二甲基 - 噻唑-2-基)-2,5-二苯基 - 四唑溴铵(MTT)实验结果表明,新型聚合物降低了细胞存活率并具有显着的细胞毒性作用。坯料纳米颗粒是具有浅蓝色乳白色的液体。透射电子显微镜显示,空胶束是均匀的球体,平均尺寸为62nm,Zeta电位为-13 mV。本发明所述的新型GA介导的聚合物载体材料具有在剂量高于500μg/ mL的时间内有效地在3天内杀死人SMMC-7721癌细胞。

著录项

  • 来源
    《Journal of Materials Research》 |2020年第10期|1236-1248|共13页
  • 作者单位

    College of Pharmacy Heilongjiang University of Chinese Medicine Heilongjiang 150040 China;

    College of Pharmacy Heilongjiang University of Chinese Medicine Heilongjiang 150040 China;

    College of Pharmacy Heilongjiang University of Chinese Medicine Heilongjiang 150040 China;

    College of Pharmacy Heilongjiang University of Chinese Medicine Heilongjiang 150040 China;

    College of Pharmacy Heilongjiang University of Chinese Medicine Heilongjiang 150040 China;

    College of Pharmacy Heilongjiang University of Chinese Medicine Heilongjiang 150040 China;

    College of Pharmacy Heilongjiang University of Chinese Medicine Heilongjiang 150040 China;

    College of Pharmacy Heilongjiang University of Chinese Medicine Heilongjiang 150040 China;

    College of Pharmacy Heilongjiang University of Chinese Medicine Heilongjiang 150040 China;

    College of Pharmacy Heilongjiang University of Chinese Medicine Heilongjiang 150040 China;

    College of Pharmacy Heilongjiang University of Chinese Medicine Heilongjiang 150040 China;

  • 收录信息 美国《科学引文索引》(SCI);美国《工程索引》(EI);美国《生物学医学文摘》(MEDLINE);
  • 原文格式 PDF
  • 正文语种 eng
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