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设计和制备季铵化果胶-蒙脱土杂化膜用于药物缓释。

Design and preparation of quaternized pectin-Montmorillonite hybrid film for sustained drug release.

机构信息

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

Beijing Key Laboratory of Lignocellulosic Chemistry, Beijing Forestry University, Beijing 100083, People's Republic of China.

出版信息

Int J Biol Macromol. 2020 Jul 1;154:413-420. doi: 10.1016/j.ijbiomac.2020.03.140. Epub 2020 Mar 16.

DOI:10.1016/j.ijbiomac.2020.03.140
PMID:32194102
Abstract

Montmorillonite (MMT) presents nonocclusive lamellar structure which restricts the potential use for sustained drug release. To solve the limitation, the quaternized pectin (QP) was synthesized and firstly introduced to form QP-MMT hybrid film containing 5-FU. The Fourier transform infrared spectroscopy (FT-IR) and X-Ray diffraction (XRD) were employed to determine the variation of the functional group and crystallinity between pectin and QP. The resultant composite film was characterized by FT-IR, XRD and Field Emission Scanning Electron Microscope. The results of the characterization indicated that intercalation reaction happened in the blending process. The optimum film showed high value of drug encapsulation efficiency (36.50%) and loading efficiency (80.30%). The in vitro drug release studies revealed that the MMT significantly improved the sustained-release performance in all simulated mediums. The cumulative release rate of sample QP-MMT was all around 20% in the first half-hour in all simulated mediums and sustained increased for more than 8 h. The cytotoxicity assay was performed to prove the great biocompatibility of QP-MMT hybrid film. The present study introduced a facile route to prepare the composite film which presented sustained drug release performance.

摘要

蒙脱石(MMT)具有非闭合层状结构,限制了其在缓控释药物方面的应用。为了解决这一限制,我们合成了季铵化果胶(QP),并首次将其引入到含有 5-FU 的 QP-MMT 杂化膜中。傅里叶变换红外光谱(FT-IR)和 X 射线衍射(XRD)用于确定果胶和 QP 之间官能团和结晶度的变化。通过傅里叶变换红外光谱(FT-IR)、X 射线衍射(XRD)和场发射扫描电子显微镜对所得复合膜进行了表征。表征结果表明,在共混过程中发生了插层反应。最优膜具有较高的药物包封效率(36.50%)和载药效率(80.30%)。体外药物释放研究表明,MMT 显著改善了所有模拟介质中的缓控释性能。在所有模拟介质中,样品 QP-MMT 的累积释放率在前半小时均在 20%左右,并持续增加 8 小时以上。细胞毒性试验证明了 QP-MMT 杂化膜具有良好的生物相容性。本研究介绍了一种简便的方法来制备具有缓控释性能的复合膜。

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