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Chiral mesoporous silica nano-screws as an efficient biomimetic oral drug delivery platform through multiple topological mechanisms
Acta Pharmaceutica Sinica B ( IF 14.7 ) Pub Date : 2021-08-18 , DOI: 10.1016/j.apsb.2021.08.014
Yumei Wang 1 , Jia Ke 1 , Xianmou Guo 1 , Kaijun Gou 1 , Zhentao Sang 2 , Yanbu Wang 1, 2 , Yan Bian 2 , Sanming Li 1 , Heran Li 2
Affiliation  

In the microscale, bacteria with helical body shapes have been reported to yield advantages in many bio-processes. In the human society, there are also wisdoms in knowing how to recognize and make use of helical shapes with multi-functionality. Herein, we designed atypical chiral mesoporous silica nano-screws (CMSWs) with ideal topological structures (e.g., small section area, relative rough surface, screw-like body with three-dimension chirality) and demonstrated that CMSWs displayed enhanced bio-adhesion, mucus-penetration and cellular uptake (contributed by the macropinocytosis and caveolae-mediated endocytosis pathways) abilities compared to the chiral mesoporous silica nanospheres (CMSSs) and chiral mesoporous silica nanorods (CMSRs), achieving extended retention duration in the gastrointestinal (GI) tract and superior adsorption in the blood circulation (up to 2.61- and 5.65-times in AUC). After doxorubicin (DOX) loading into CMSs, DOX@CMSWs exhibited controlled drug release manners with pH responsiveness in vitro. Orally administered DOX@CMSWs could efficiently overcome the intestinal epithelium barrier (IEB), and resulted in satisfactory oral bioavailability of DOX (up to 348%). CMSWs were also proved to exhibit good biocompatibility and unique biodegradability. These findings displayed superior ability of CMSWs in crossing IEB through multiple topological mechanisms and would provide useful information on the rational design of nano-drug delivery systems.



中文翻译:

手性介孔二氧化硅纳米螺钉通过多种拓扑机制作为高效的仿生口服给药平台

据报道,在微观尺度上,具有螺旋体形状的细菌在许多生物过程中具有优势。在人类社会中,懂得如何识别和利用多功能的螺旋形状也有智慧。在此,我们设计了具有理想拓扑结构(例如,小截面面积,相对粗糙的表面,具有三维手性的螺旋状体)并证明与手性介孔二氧化硅纳米球 (CMSSs) 和手性介孔二氧化硅纳米棒 (CMSRs),可延长在胃肠道 (GI) 的保留时间,并在血液循环中具有出色的吸附性(AUC 高达 2.61 倍和 5.65 倍)。在多柔比星 (DOX) 负载 CMS 后,DOX@CMSWs在体外表现出具有 pH 响应性的受控药物释放方式. 口服 DOX@CMSWs 可有效克服肠上皮屏障 (IEB),并导致 DOX 的口服生物利用度令人满意(高达 348%)。CMSWs 也被证明具有良好的生物相容性和独特的生物降解性。这些发现显示了 CMSW 通过多种拓扑机制跨越 IEB 的卓越能力,并将为纳米药物递送系统的合理设计提供有用的信息。

更新日期:2021-08-18
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