Abstract Mesoporous silica nanoparticles (MSNs) carrying gatekeepers that are stimuli-responsive are widely investigated for the controlled delivery of drug at target sites. In this study, thioketal (TK) functionalized methoxy poly(ethylene glycol) (mPEG-TK) as ROS-responsive gatekeeper is used to modify MSNs and leads to a reactive oxygen species (ROS)-responsive delivery for antibacterial drug. Vancomycin (Van) was taken as the antibacterial drug and then physically encapsulated into the surface amino functionalized MSNs (N-MSNs). Subsequently, mPEG-TK was surface immobilized. Van loaded N-MSNs with surface modification of mPEG-TK (Van-mPEG-TK-MSNs) presented approximately 21% release of Van in a physiological environment in 36 h. With H2O2 increasing in the medium, the release rate of Van from Van-mPEG-TK-MSNs was significantly up-regulated following gatekeepers' disintegration. When Van-mPEG-TK-MSNs was applied in vivo, the infected site was fully cleared after 14 days and the tissue was free of infection. On the whole, the mentioned results suggested that Van-mPEG-TK-MSNs could act as a potential antimicrobial. This study can broaden MSNs' applications and advance the development of novel antibacterial agents.

中文翻译：

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活性氧敏感性硫缩酮连接介孔二氧化硅纳米粒子作为药物载体的有效抗菌活性

摘要 介孔二氧化硅纳米粒子 (MSN) 携带刺激响应的看门人，被广泛研究用于在靶点控制药物递送。在这项研究中，硫缩酮 (TK) 功能化的甲氧基聚乙二醇 (mPEG-TK) 作为 ROS 响应性看门人用于修饰 MSN，并导致抗菌药物的活性氧 (ROS) 响应性递送。以万古霉素（Van）为抗菌药物，物理包裹在表面氨基功能化的MSNs（N-MSNs）中。随后，mPEG-TK 被表面固定。经 mPEG-TK 表面修饰的 Van 负载 N-MSNs (Van-mPEG-TK-MSNs) 在生理环境中在 36 小时内释放了约 21% 的 Van。随着介质中 H2O2 的增加，Van-mPEG-TK-MSNs 中 Van 的释放速率在守门人解体后显着上调。Van-mPEG-TK-MSNs在体内应用时，感染部位在14天后完全清除，组织没有感染。总的来说，上述结果表明 Van-mPEG-TK-MSNs 可以作为潜在的抗菌剂。这项研究可以拓宽 MSN 的应用范围并推动新型抗菌剂的开发。