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载阿莫西林尼奥斯omes 的制备和优化:增加抗菌和抗生物膜作用的多药耐药菌株的适当策略。

Fabrication and optimization of amoxicillin-loaded niosomes: an appropriate strategy to increase antimicrobial and anti-biofilm effects against multidrug-resistant  strains.

机构信息

Department of Microbiology, Faculty of Advanced Science and Technology, Tehran Medical Sciences, Islamic Azad University, Tehran, Iran.

Department of Biology, Parand Branch, Islamic Azad University, Parand, Iran.

出版信息

Drug Dev Ind Pharm. 2021 Oct;47(10):1568-1577. doi: 10.1080/03639045.2022.2027958. Epub 2022 Jan 19.

DOI:10.1080/03639045.2022.2027958
PMID:35007176
Abstract

In this study, different formulations of amoxicillin-loaded niosomes were fabricated using the thin-film hydration method and their physicochemical properties were determined using scanning electron microscopy (SEM), dynamic light scattering (DLS), and Fourier-transform infrared (FTIR) spectroscopy. The optimum prepared niosomes had a spherical morphology with an average size of 170.6 ± 6.8 nm and encapsulation efficiency of 65.78 ± 1.45%. The drug release study showed that the release rate of amoxicillin from niosome containing amoxicillin was slow and 47 ± 1% of the drug was released within 8 h, while 97 ± 0.5% of the free drug was released. In addition, amoxicillin-loaded niosome increased the antimicrobial activity by 2-4 folds against multidrug-resistant (MDR) strains using broth microdilution assay. Moreover, at 1/2 minimum inhibitory concentrations, amoxicillin-loaded niosome significantly enhanced the anti-biofilm activity compared to free amoxicillin. Amoxicillin-loaded niosome had negligible cytotoxicity against HEK-293 normal cell line compared to free amoxicillin. The free niosomes exhibited no toxicity against HEK-293 cells and presented a biocompatible nanoscale delivery system. Based on the results, it can be concluded that amoxicillin-loaded niosome can be used as a promising candidate for enhancing antimicrobial and anti-biofilm effects against MDR strains of .

摘要

在这项研究中,使用薄膜水化法制备了不同配方的阿莫西林载入尼奥斯omes,并通过扫描电子显微镜(SEM)、动态光散射(DLS)和傅里叶变换红外(FTIR)光谱法测定其理化性质。最佳制备的尼奥斯omes 具有球形形态,平均粒径为 170.6±6.8nm,包封效率为 65.78±1.45%。药物释放研究表明,含阿莫西林的尼奥斯ome 中阿莫西林的释放速度较慢,8 小时内释放了 47±1%的药物,而游离药物释放了 97±0.5%。此外,用肉汤微量稀释法测定,阿莫西林载入尼奥斯ome 可将多药耐药(MDR)菌株的抗菌活性提高 2-4 倍。此外,在 1/2 最低抑菌浓度下,与游离阿莫西林相比,阿莫西林载入尼奥斯ome 显著增强了抗生物膜活性。与游离阿莫西林相比,阿莫西林载入尼奥斯ome 对 HEK-293 正常细胞系的细胞毒性可忽略不计。游离尼奥斯ome 对 HEK-293 细胞无毒性,呈现出生物相容性的纳米级给药系统。基于这些结果,可以得出结论,阿莫西林载入尼奥斯ome 可用作增强抗菌和抗生物膜作用的有前途的候选物,可用于治疗多药耐药株。

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