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基于果胶/修饰纳米碳球纳米复合凝胶膜的新型简单口服结肠定位给药系统。

A novel and simple oral colon-specific drug delivery system based on the pectin/modified nano-carbon sphere nanocomposite gel films.

机构信息

College of Chemical Engineering, Xinjiang Agricultural University, Urumchi 830052, Xinjiang, People's Republic of China.

College of Chemical Engineering, Xinjiang Agricultural University, Urumchi 830052, Xinjiang, People's Republic of China.

出版信息

Int J Biol Macromol. 2020 Aug 15;157:170-176. doi: 10.1016/j.ijbiomac.2020.04.197. Epub 2020 Apr 26.

Abstract

The 3-aminopropyltriethoxysilane modified nano-carbon sphere (MNCS) was added into pectin-Ca film to improve the controlled release properties of the pectin-based oral colon-specific drug delivery system (OCDDS). The FT-IR measurements indicated the successful modification of nano-carbon sphere via silylation reaction and the electrostatic interaction between the pectin molecules and MNCS in the composite film. The FE-SEM showed the pore structure when the MNCS was mingled with the pectin. The 5-fluorouracil (5-FU) was employed as the drug model and the controlled release properties of the corresponding OCDDSs were determined. The values of the encapsulation efficiency ranged from 30.1% to 52.6%. All composite film based OCDDSs presented higher encapsulation efficiency than single pectin-Ca based OCDDS. The drug release studies emerged that almost all the OCDDSs from composite films presented better release properties than single pectin-Ca based OCDDS. The sample C revealed best release performance with the cumulative release rate of 32.17%, 22.77% and 63.89% in the simulated gastric fluid, small intestinal fluid and colon fluid, respectively. In addition, the kinetics studies were performed to analyze the release data. The cytotoxicity assay indicated good biocompatibility of the composite carriers.

摘要

3-氨丙基三乙氧基硅烷改性纳米碳球(MNCS)被添加到果胶-Ca 膜中,以改善果胶基口服结肠靶向给药系统(OCDDS)的控制释放性能。FT-IR 测量表明,纳米碳球通过硅烷化反应成功修饰,并且在复合膜中果胶分子与 MNCS 之间存在静电相互作用。FE-SEM 显示了 MNCS 与果胶混合时的孔结构。将 5-氟尿嘧啶(5-FU)用作药物模型,并测定相应 OCDDS 的控制释放性能。包封效率值范围为 30.1%至 52.6%。所有基于复合膜的 OCDDS 的包封效率均高于单一果胶-Ca 基 OCDDS。药物释放研究表明,所有基于复合膜的 OCDDS 都表现出比单一果胶-Ca 基 OCDDS 更好的释放性能。样品 C 在模拟胃液、小肠液和结肠液中的累积释放率分别为 32.17%、22.77%和 63.89%,表现出最佳的释放性能。此外,还进行了动力学研究来分析释放数据。细胞毒性试验表明复合载体具有良好的生物相容性。

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