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一锅法合成 α-亚麻酸纳米乳液模板载药硅介孔复合材料作为抗耐药结核分枝杆菌的高效杀菌剂。

One-pot synthesis of α-Linolenic acid nanoemulsion-templated drug-loaded silica mesocomposites as efficient bactericide against drug-resistant Mycobacterium tuberculosis.

机构信息

Center for Global Health, School of Public Health, Nanjing Medical University, Nanjing 211166, China.

Center for Global Health, School of Public Health, Nanjing Medical University, Nanjing 211166, China; Department of Chronic Communicable Disease, Center for Disease Control and Prevention of Jiangsu Province, Nanjing, China.

出版信息

Eur J Pharm Sci. 2022 Sep 1;176:106261. doi: 10.1016/j.ejps.2022.106261. Epub 2022 Jul 15.

Abstract

Nowadays, pathogenic infection has posed a severe threat to the public health and environmental sanitation, urging a continuous search of efficacious and safe bactericidal agents of various formulated forms. Here, a facile one-pot hydrothermal preparation of mesoporous silica nanoparticles using ultrasonication-assisted nanoemulsion of α-Linolenic acid (α-LA) as template was developed. The formed silica mesocomposite at water/fatty-acid surface provides an easy yet green synthesis route, which can be generalized for the further encapsulation of hydrophobic drugs such as antimycobacterial Rifampicin (RIF). The obtained α-LA nanoemulsion-templated silica nanoparticles (LNS NPs), with a weight content of ∼17% α-LA in the composite, showed apparent antibacterial effect against Staphylococcus aureus (S. aureus). By comparison, the removal of α-LA from the silica nanoparticles (LNS-1 NPs) resulted in the composite of enlarged pore size with negligible bactericidal activities. Notably, the Isoniazide (INH) and Rifampicin (RIF)-encapsulated LNS NPs exhibited outstanding antimycobacterial activity against both drug-sensitive and drug-resistant Mycobacterium tuberculosis (M. tuberculosis). The obtained highly biocompatible, biosafe and low-energy consumptive α-LA-contained mesostructured silica-based bactericide holds promising therapeutic potentials to tackle the emerging drug-resistant infectious microbes.

摘要

如今,病原感染对公共卫生和环境卫生构成了严重威胁,促使人们不断寻找各种剂型的有效且安全的杀菌剂。在这里,我们开发了一种简便的一锅水热法,使用超声辅助的 α-亚麻酸(α-LA)纳米乳液作为模板制备介孔二氧化硅纳米粒子。在水/脂肪酸表面形成的硅介孔复合材料提供了一种简单而绿色的合成途径,可进一步封装疏水性药物,如抗分枝杆菌的利福平(RIF)。所获得的 α-LA 纳米乳液模板化二氧化硅纳米粒子(LNS NPs),在复合材料中具有约 17%的 α-LA 重量含量,对金黄色葡萄球菌(S. aureus)表现出明显的抗菌作用。相比之下,从二氧化硅纳米粒子(LNS-1 NPs)中去除 α-LA 会导致复合物体积增大,而抗菌活性可忽略不计。值得注意的是,异烟肼(INH)和利福平(RIF)包封的 LNS NPs 对敏感和耐药结核分枝杆菌(M. tuberculosis)均表现出出色的抗分枝杆菌活性。所获得的高度生物相容、生物安全且能耗低的含 α-LA 的介孔结构基于二氧化硅的杀菌剂具有治疗新兴耐药性感染微生物的巨大潜力。

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