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载抗生素聚乳酸纳米颗粒的合成及其对大肠杆菌O157:H7和耐甲氧西林金黄色葡萄球菌的抗菌活性

[Synthesis of antibiotic loaded polylactic acid nanoparticles and their antibacterial activity against Escherichia coli O157:H7 and methicillin-resistant Staphylococcus aureus].

作者信息

Herrera Mónica Tatiana, Artunduaga Jhon Jhamilton, Ortiz Claudia Cristina, Torres Rodrigo Gonzalo

机构信息

Escuela de Química, Universidad Industrial de Santander, Bucaramanga, Colombia.

出版信息

Biomedica. 2017 Jan 24;37(1):11-21. doi: 10.7705/biomedica.v37i1.2995.

Abstract

INTRODUCTION

Polymeric nanoparticles are promising nanotechnology tools to fight pathogenic bacteria resistant to conventional antibiotics.

OBJECTIVE

To synthesize polylactic acid nanoparticles loaded with ofloxacin and vancomycin, and to determine their antibacterial activity against Escherichia coli O157:H7 and methicillin-resistant Staphylococcus aureus (MRSA).

MATERIALS AND METHODS

We synthesized ofloxacin or vancomycin loaded polylactic acid nanoparticles by the emulsification-solvent evaporation method, and characterized them by dynamic light scattering, laser Doppler electrophoresis and scanning electron microscopy. We evaluated in vitro antibacterial activity of ofloxacin- and vancomycin-loaded polylactic acid nanoparticles against E. coli O157:H7 and MRSA using the broth microdilution method.

RESULTS

Ofloxacin- and vancomycin-loaded polylactic acid nanoparticles registered a positive surface charge density of 21 mV and an average size lower than 379 nm. In vitro minimum inhibitory concentration (MIC50) of ofloxacin-polylactic acid nanoparticles was 0,001 μg/ml against E. coli O157:H7, i.e., 40 times lower than the free ofloxacin (MIC50: 0.04 μg/ml), indicating enhanced antibacterial activity while the in vitro MIC50 of vancomycin-polylactic acid nanoparticles was 0,005 μg/ml against MRSA, i.e., 100 times lower than that of free vancomycin (MIC50: 0.5 μg/ml).

CONCLUSION

Polylactic acid nanoparticles loaded with ofloxacin and vancomycin showed a higher antibacterial activity. Polymeric nanoparticles are a possible alternative for drug design against pathogenic bacterial strains of public health interest.

摘要

引言

聚合物纳米颗粒是对抗耐传统抗生素的致病细菌的有前景的纳米技术工具。

目的

合成负载氧氟沙星和万古霉素的聚乳酸纳米颗粒,并测定其对大肠杆菌O157:H7和耐甲氧西林金黄色葡萄球菌(MRSA)的抗菌活性。

材料与方法

我们通过乳化溶剂蒸发法合成了负载氧氟沙星或万古霉素的聚乳酸纳米颗粒,并通过动态光散射、激光多普勒电泳和扫描电子显微镜对其进行表征。我们使用肉汤微量稀释法评估了负载氧氟沙星和万古霉素的聚乳酸纳米颗粒对大肠杆菌O157:H7和MRSA的体外抗菌活性。

结果

负载氧氟沙星和万古霉素的聚乳酸纳米颗粒的表面电荷密度为21 mV,平均尺寸小于379 nm。氧氟沙星-聚乳酸纳米颗粒对大肠杆菌O157:H7的体外最低抑菌浓度(MIC50)为0.001 μg/ml,即比游离氧氟沙星(MIC50: 0.04 μg/ml)低40倍,表明抗菌活性增强,而万古霉素-聚乳酸纳米颗粒对MRSA的体外MIC50为0.005 μg/ml,即比游离万古霉素(MIC50: 0.5 μg/ml)低100倍。

结论

负载氧氟沙星和万古霉素的聚乳酸纳米颗粒显示出更高的抗菌活性。聚合物纳米颗粒是针对具有公共卫生意义的致病细菌菌株进行药物设计的一种可能替代方案。

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