{"title":"评估负载莫西沙星的固体脂质纳米颗粒的细菌吸收、对大肠杆菌的抗菌效果和细胞毒性作用。","authors":"Merve Eylul Kiymaci, Gizem Ruya Topal, Ozgur Esim, Merve Bacanli, Cansel Kose Ozkan, Onur Erdem, Ayhan Savaser, Yalcin Ozkan","doi":"10.2478/aiht-2022-73-3667","DOIUrl":null,"url":null,"abstract":"<p><p>Moxifloxacin (MOX) is an important antibiotic commonly used in the treatment of recurrent <i>Escherichia coli (E. coli)</i> infections. The aim of this study was to investigate its antibacterial efficiency when used with solid lipid nanoparticles (SNLs) and nanostructured lipid carriers (NLCs) as delivery vehicles. For this purpose we designed two SLNs (SLN1 and SLN2) and two NLCs (NLC1 and NLC2) of different characteristics (particle size, size distribution, zeta potential, and encapsulation efficiency) and loaded them with MOX to determine its release, antibacterial activity against <i>E. coli</i>, and their cytotoxicity to the RAW 264.7 monocyte/macrophage-like cell line <i>in vitro</i>. With bacterial uptake of 57.29 %, SLN1 turned out to be significantly more effective than MOX given as standard solution, whereas SLN2, NLC1, and NLC2 formulations with respective bacterial uptakes of 50.74 %, 39.26 %, and 32.79 %, showed similar activity to standard MOX. Cytotoxicity testing did not reveal significant toxicity of nanoparticles, whether MOX-free or MOX-loaded, against RAW 264.7 cells. Our findings may show the way for a development of effective lipid carriers that reduce side effects and increase antibacterial treatment efficacy in view of the growing antibiotic resistance.</p>","PeriodicalId":55462,"journal":{"name":"Arhiv Za Higijenu Rada I Toksikologiju-Archives of Industrial Hygiene and Toxicology","volume":"73 4","pages":"260-269"},"PeriodicalIF":1.7000,"publicationDate":"2022-12-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://ftp.ncbi.nlm.nih.gov/pub/pmc/oa_pdf/4f/7d/aiht-73-260.PMC9985348.pdf","citationCount":"0","resultStr":"{\"title\":\"Evaluation of bacterial uptake, antibacterial efficacy against <i>Escherichia coli</i>, and cytotoxic effects of moxifloxacin-loaded solid lipid nanoparticles.\",\"authors\":\"Merve Eylul Kiymaci, Gizem Ruya Topal, Ozgur Esim, Merve Bacanli, Cansel Kose Ozkan, Onur Erdem, Ayhan Savaser, Yalcin Ozkan\",\"doi\":\"10.2478/aiht-2022-73-3667\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p><p>Moxifloxacin (MOX) is an important antibiotic commonly used in the treatment of recurrent <i>Escherichia coli (E. coli)</i> infections. 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引用次数: 0
摘要
莫西沙星(MOX)是一种重要的抗生素,常用于治疗复发性大肠杆菌(E. coli)感染。本研究的目的是调查莫西沙星与固体脂质纳米颗粒(SNLs)和纳米结构脂质载体(NLCs)一起作为递送载体时的抗菌效率。为此,我们设计了两种具有不同特性(粒度、粒度分布、ZETA电位和封装效率)的SLN(SLN1和SLN2)和两种NLC(NLC1和NLC2),并将MOX载入其中,在体外测定其释放、对大肠杆菌的抗菌活性以及对RAW 264.7单核/巨噬细胞样细胞系的细胞毒性。结果表明,SLN1 的细菌吸收率为 57.29%,明显比作为标准溶液的 MOX 更有效;而 SLN2、NLC1 和 NLC2 配方的细菌吸收率分别为 50.74%、39.26% 和 32.79%,显示出与标准 MOX 相似的活性。细胞毒性测试表明,无论是不含 MOX 还是含有 MOX 的纳米颗粒,对 RAW 264.7 细胞都没有明显毒性。鉴于抗生素耐药性的不断增加,我们的研究结果可能会为开发有效的脂质载体指明方向,从而减少副作用并提高抗菌治疗效果。
Evaluation of bacterial uptake, antibacterial efficacy against Escherichia coli, and cytotoxic effects of moxifloxacin-loaded solid lipid nanoparticles.
Moxifloxacin (MOX) is an important antibiotic commonly used in the treatment of recurrent Escherichia coli (E. coli) infections. The aim of this study was to investigate its antibacterial efficiency when used with solid lipid nanoparticles (SNLs) and nanostructured lipid carriers (NLCs) as delivery vehicles. For this purpose we designed two SLNs (SLN1 and SLN2) and two NLCs (NLC1 and NLC2) of different characteristics (particle size, size distribution, zeta potential, and encapsulation efficiency) and loaded them with MOX to determine its release, antibacterial activity against E. coli, and their cytotoxicity to the RAW 264.7 monocyte/macrophage-like cell line in vitro. With bacterial uptake of 57.29 %, SLN1 turned out to be significantly more effective than MOX given as standard solution, whereas SLN2, NLC1, and NLC2 formulations with respective bacterial uptakes of 50.74 %, 39.26 %, and 32.79 %, showed similar activity to standard MOX. Cytotoxicity testing did not reveal significant toxicity of nanoparticles, whether MOX-free or MOX-loaded, against RAW 264.7 cells. Our findings may show the way for a development of effective lipid carriers that reduce side effects and increase antibacterial treatment efficacy in view of the growing antibiotic resistance.
期刊介绍:
Archives of Industrial Hygiene and Toxicology (abbr. Arh Hig Rada Toksikol) is a peer-reviewed biomedical scientific quarterly that publishes contributions relevant to all aspects of environmental and occupational health and toxicology.