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载替考拉宁适体靶向 PLGA 纳米粒对金黄色葡萄球菌的抑制作用。

Inhibitory effects of aptamer targeted teicoplanin encapsulated PLGA nanoparticles for Staphylococcus aureus strains.

机构信息

Department of Molecular Biology and Genetics, Yildiz Technical University, Istanbul, Turkey.

School of Medicine, Altinbas University, Istanbul, Turkey.

出版信息

World J Microbiol Biotechnol. 2020 Apr 25;36(5):69. doi: 10.1007/s11274-020-02845-y.

DOI:10.1007/s11274-020-02845-y
PMID:32333113
Abstract

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.

摘要

传统抗生素治疗方法出现耐药性,因此需要替代的给药系统。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)。应对抗生素耐药性发展的一种策略是在治疗过程中限制剂量和用量。抗生素靶向递送系统被认为是一种减缓耐药性发展并提高已耐药病原体对抗微生物药物效率的机制。在这项研究中,我们报告了聚乳酸-共-羟基乙酸(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功能化。对于敏感株,替考拉宁的最低抑菌浓度(MIC)值降低了 32 倍,对于中度耐药的临床耐甲氧西林金黄色葡萄球菌分离株,用适体-PLGA 纳米颗粒进行替考拉宁治疗后,MIC 值降低了约 64 倍。虽然未经靶向的 PLGA 纳米颗粒中的替考拉宁递送使金黄色葡萄球菌和表皮葡萄球菌的敏感株的 MIC 值降低了 8 倍,使耐药株的 MIC 值降低了 2 倍,但适体的靶向特异性降低了金黄色葡萄球菌的 MIC 值,而不是表皮葡萄球菌的 MIC 值。因此,抗生素的适体靶向 PLGA 递药可能是对抗一些多药耐药细菌病原体的一种有吸引力的替代方法。

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