摘要

       我们描述了一种基于磁性纳米粒子（NPs）结合细胞穿透肽（CPP）的新型抗生素给药系统。采用共沉积法制备了二氧化硅包覆的氧化铁纳米颗粒，并通过物理化学结合将其包覆在聚乙烯醇（PVA）聚合物网络中。万古霉素（Vancomycin，VAN）被包埋在PVA网络中。在固相合成了一个六肽序列Gly-Ala-Phe-Pro-His-Arg，并将其与磁性纳米粒子表面结合。通过精密分析，监测药物在载体系统中的掺入率和药物释放。共聚焦显微镜显示NPs可以内化到金黄色葡萄球菌和大肠杆菌的细菌细胞中。低剂量的VAN能显著增强VAN的抗菌作用。优点包括快速靶向给药过程，减少药物剂量，对革兰氏阳性菌和革兰氏阴性菌的作用相等。

        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.

         https://pubs.rsc.org/en/content/articlelanding/2020/NR/C9NR09687F#!divAbstract