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通过将穿透细胞肽偶联到杂交磁性纳米粒子中,增强万古霉素的活性。

Enhanced activity of vancomycin by encapsulation in hybrid magnetic nanoparticles conjugated to a cell-penetrating peptide.

机构信息

Department of Nuclear Medicine, West China Hospital, Sichuan University, No. 37, Guoxue Alley, Chengdu 610041, Sichuan Province, P.R. China.

Catalysts and Organic Synthesis Research Laboratory, Department of Chemistry, Iran University of Science and Technology, Tehran 16846-13114, Iran.

出版信息

Nanoscale. 2020 Feb 14;12(6):3855-3870. doi: 10.1039/c9nr09687f. Epub 2020 Jan 30.

Abstract

We describe a novel antibiotic delivery system based on magnetic nanoparticles (NPs) conjugated to a cell-penetrating peptide (CPP). Silica-coated iron oxide NPs were produced via a co-deposition method, and coated by a polyvinyl alcohol (PVA) polymeric network via physicochemical binding. Vancomycin (VAN) was then entrapped into this PVA network. A hexapeptide sequence Gly-Ala-Phe-Pro-His-Arg, was synthesized in the solid phase and then conjugated onto the surface of the magnetic NPs. The drug ratio incorporation into the carrier system and drug release were monitored through precise analysis. Confocal microscopy showed that the NPs could be internalized into Staphylococcus aureus and Escherichia coli bacterial cells. The antimicrobial effects of VAN were significantly enhanced by this system with a low dosage of VAN. Advantages include rapid targeted-drug delivery process, drug dose reduction, and equal effects on both Gram-positive and Gram-negative bacteria.

摘要

我们描述了一种基于磁性纳米粒子(NPs)与穿透肽(CPP)结合的新型抗生素输送系统。通过共沉积法制备了二氧化硅包覆的氧化铁 NPs,并通过物理化学结合被聚乙烯醇(PVA)聚合物网络包覆。万古霉素(VAN)随后被包埋在这个 PVA 网络中。一个六肽序列 Gly-Ala-Phe-Pro-His-Arg 通过固相合成,然后连接到磁性 NPs 的表面。通过精确分析监测药物与载体系统的结合比和药物释放。共聚焦显微镜显示,NPs 可以被内化到金黄色葡萄球菌和大肠杆菌细菌细胞中。与低剂量 VAN 相比,该系统显著增强了 VAN 的抗菌作用。其优点包括快速靶向药物输送过程、减少药物剂量以及对革兰氏阳性菌和革兰氏阴性菌的同等作用。

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