Chiral microenvironment-responsive mesoporous silica nanoparticles for delivering indometacin with chiral recognition function

Materials & Design

Xianmou Guo¹  Yuxin Wang²  Yumei Wang³  Heran Li³  Sanming Li³  Shuangshuang Ma³  Zhentao Sang³  Linlin Xie³  Yingyu Guo⁴  Kaijun Gou⁴ 

[1] College of Pharmacy, Southwest Minzu University, Wuhou RD16, 610041, Chengdu, Sichuan Province, China, Department of Pharmaceutics, School of Pharmacy, Shenyang Pharmaceutical University, Wenhua RD103, 110016 Shenyang, Liaoning Province, China;Department of Pharmaceutics, School of Pharmacy, Shenyang Pharmaceutical University, Wenhua RD103, 110016 Shenyang, Liaoning Province, China;Department of Pharmaceutics, School of Pharmacy, Shenyang Pharmaceutical University, Wenhua RD103, 110016 Shenyang, Liaoning Province, China;School of Pharmacy, China Medical University, Puhe RD77, 110122, Shenyang North New Area, Shenyang, Liaoning Province, China;

关键词: Chiral microenvironment-response;    High specific surface area;    Chiral recognition;    Biological effects;    Indometacin;   

DOI  :  

来源: DOAJ

【 摘 要 】

The purpose of this study was to investigate the potential chiral recognition functions induced by two kinds of novel chiral microenvironment-responsive mesoporous silica nanoparticles (CMR-L-MSN and CMR-D-MSN) for the oral delivery of the poorly water-soluble achiral drug indomethacin (IMC). The as-synthesized CMR-L-MSN and CMR-D-MSN with molecular chirality and high specific surface area (SBET: 1141 and 1075 m2/g, respectively) were successfully prepared through grafting chiral molecular functional groups. The characterization results showed that CMR-L-MSN and CMR-D-MSN were spherical nanoparticles with opposite chiral features and clearly visible pore channels. Meanwhile, they exhibited good biosafety and degradability. In vitro drug release study indicated that both CMR-L-MSN and CMR-D-MSN significantly improved IMC dissolution compared with naked-MSN (N-MSN) (p < 0.05) and exhibited different chiral recognition functions for drug release in the simulated chiral environments in vitro (pH 6.8 PBS-D/L), in which CMR-D-MSN could be triggered by the L-configurations in chiral environments and exhibited a better drug release effect. As expect, the results of in vivo biological effects disclosed that CMR-D-MSN had higher bioavailability of IMC and obvious advantages on drug adsorption and in vivo distribution, and exerted stronger anti-inflammatory effect after making specific response to the in vivo chiral environment.

【 授权许可】

Unknown