Emergence of resistance to traditional antibiotic treatments necessitates alternative delivery systems. Teicoplanin is a glycopeptide antibiotic used in the treatments of serious infections caused by Gram-positive bacteria, including Methicillin Resistant Staphylococcus aureus (MRSA). One strategy to keep up with antibiotic resistance development is to limit dose and amount during treatments. Targeted delivery systems of antibiotics have been suggested as a mechanism to slow-down the evolution of resistance and to increase efficiency of the antimicrobials on already resistant pathogens. In this study, we report teicoplanin delivery nanoparticles of Poly Lactic-co-Glycolic Acid (PLGA), which are functionalized with S. aureus specific aptamers. A 32-fold decrease in minimum inhibitory concentration (MIC) values of teicoplanin for S. aureus was demonstrated for susceptible strains and about 64-fold decline in MIC value was achieved for moderately resistant clinical isolates of MRSA upon teicoplanin treatment with aptamer-PLGA nanoparticles. Although teicoplanin delivery in PLGA nanoparticles without targeting demonstrated eightfold decrease in MIC of susceptible strains of S. aureus and S. epidermidis and twofold in MIC of resistant strains, the aptamer targeting specifically decreased MIC for S. aureus, but not for S. epidermidis. Therefore, aptamer-targeted PLGA delivery of antibiotic can be an attractive alternative to combat with some of the multi-drug resistant bacterial pathogens.

中文翻译：

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适配体靶向替考拉宁包裹的PLGA纳米颗粒对金黄色葡萄球菌菌株的抑制作用

对传统抗生素治疗的耐药性的出现需要替代递送系统。替考拉宁是一种糖肽类抗生素，用于治疗由革兰氏阳性菌引起的严重感染，包括耐甲氧西林金黄色葡萄球菌 (MRSA)。跟上抗生素耐药性发展的一种策略是在治疗期间限制剂量和数量。已经建议将抗生素靶向递送系统作为减缓耐药性演变和提高抗菌剂对已经耐药病原体的效率的一种机制。在这项研究中，我们报告了聚乳酸-共-乙醇酸 (PLGA) 的替考拉宁递送纳米颗粒，其用金黄色葡萄球菌特异性适体进行了功能化。替考拉宁对金黄色葡萄球菌的最低抑菌浓度 (MIC) 值降低了 32 倍。金黄色葡萄球菌在敏感菌株中得到证实，并且在用适体-PLGA 纳米颗粒处理替考拉宁后，中度耐药的 MRSA 临床分离株的 MIC 值下降了约 64 倍。虽然替考拉宁在 PLGA 纳米颗粒中的递送没有靶向，证明金黄色葡萄球菌和表皮葡萄球菌的敏感菌株的 MIC 降低了八倍，耐药菌株的 MIC 降低了两倍，但靶向适体专门降低了金黄色葡萄球菌的 MIC，但不会降低表皮葡萄球菌的 MIC。因此，以适体为目标的 PLGA 递送抗生素可以成为对抗某些多重耐药细菌病原体的有吸引力的替代方案。虽然替考拉宁在 PLGA 纳米颗粒中的递送没有靶向，证明金黄色葡萄球菌和表皮葡萄球菌的敏感菌株的 MIC 降低了八倍，耐药菌株的 MIC 降低了两倍，但靶向适体专门降低了金黄色葡萄球菌的 MIC，但不会降低表皮葡萄球菌的 MIC。因此，以适体为目标的 PLGA 递送抗生素可以成为对抗某些多重耐药细菌病原体的有吸引力的替代方案。虽然替考拉宁在 PLGA 纳米颗粒中的递送没有靶向，证明金黄色葡萄球菌和表皮葡萄球菌的敏感菌株的 MIC 降低了八倍，耐药菌株的 MIC 降低了两倍，但靶向适体专门降低了金黄色葡萄球菌的 MIC，但不会降低表皮葡萄球菌的 MIC。因此，以适体为目标的 PLGA 递送抗生素可以成为对抗某些多重耐药细菌病原体的有吸引力的替代方案。