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具有手性识别功能的口服递送吲哚美辛的隐藏体介孔硅纳米粒子。

Concealed body mesoporous silica nanoparticles for orally delivering indometacin with chiral recognition function.

机构信息

Wuya College of Innovation, Shenyang Pharmaceutical University, Wenhua road 103, Shenyang, China.

Academic Department, Chinese Pharmaceutical Association, Jianwai SOHO, No.4 Jianwai Street, Chaoyang District, Beijing, China.

出版信息

Mater Sci Eng C Mater Biol Appl. 2018 Sep 1;90:314-324. doi: 10.1016/j.msec.2018.04.071. Epub 2018 Apr 26.

Abstract

The primary purpose of this research was to explore the potential chiral recognition functions induced by two kinds of novel concealed body mesoporous silica nanoparticles (Cb-D-MSN and Cb-L-MSN) with the entrapment of indometacin (IMC). The as-synthesized Cb-D-MSN and Cb-L-MSN were successfully fabricated through grafting molecular functional groups. The TEM result showed that Cb-D-MSN and Cb-L-MSN were regular spheres with concealed pore channels. Nitrogen adsorption/desorption analysis confirmed mesoporous structure of Cb-D-MSN and Cb-L-MSN. In vitro drug release study indicated that both Cb-D-MSN and Cb-L-MSN significantly improved IMC dissolution compared with Naked-MSN (N-MSN). Interestingly, the results of anti-inflammation pharmacodynamics and pharmacokinetics indicated that Cb-D-MSN and Cb-L-MSN exerted different chiral recognition functions, which Cb-D-MSN can deliver more IMC evidenced by molecular simulations. It is expected that the herein favorable carriers with unique advantages in triggering chiral biological environment can be promising for constructing drug delivery system.

摘要

本研究的主要目的是探索两种新型隐藏体介孔硅纳米粒子(Cb-D-MSN 和 Cb-L-MSN)与吲哚美辛(IMC)包埋后可能产生的手性识别功能。所合成的 Cb-D-MSN 和 Cb-L-MSN 通过接枝分子官能团成功制备。TEM 结果表明,Cb-D-MSN 和 Cb-L-MSN 是具有隐藏孔道的规则球体。氮吸附/解吸分析证实了 Cb-D-MSN 和 Cb-L-MSN 的介孔结构。体外药物释放研究表明,与裸介孔硅纳米粒子(N-MSN)相比,Cb-D-MSN 和 Cb-L-MSN 均显著提高了 IMC 的溶解度。有趣的是,抗炎药效学和药代动力学的结果表明,Cb-D-MSN 和 Cb-L-MSN 发挥了不同的手性识别功能,分子模拟表明 Cb-D-MSN 可以输送更多的 IMC。预计这些具有独特优势的载体能够在触发手性生物环境方面具有广阔的前景,有望构建药物输送系统。

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