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菠萝蛋白酶包裹的金纳米颗粒作为新型药物递送载体以增强抗生素左氧氟沙星的效果。

Bromelain capped gold nanoparticles as the novel drug delivery carriers to aggrandize effect of the antibiotic levofloxacin.

作者信息

Bagga Paramdeep, Ansari Tarique Mahmood, Siddiqui Hefazat Hussain, Syed Asad, Bahkali Ali H, Rahman Md Azizur, Khan Mohd Sajid

机构信息

Department of Pharmacy, Integral University, Lucknow, Uttar Pradesh 226026 (India).

Botany and Microbiology Department, Faculty of Science, King Saud University, Riyadh, Saudi Arabia.

出版信息

EXCLI J. 2016 Dec 6;15:772-780. doi: 10.17179/excli2016-710. eCollection 2016.

Abstract

To develop bromelain capped gold nanoparticles (BRN capped Au-NPs) as the effective drug delivery carriers of the antibiotic levofloxacin (LvN) and evaluate antibacterial potential of its bioconjugated form compared to pure LvN. BRN capped Au-NPs were synthesized by method and bioconjugated to LvN using 1-ethyl-3-(3-dimethylamino-propyl)-carbodiimide as activator to form Au-BRN-LvN-NPs. These were characterized for mean particle size by dynamic light scattering analysis, zeta potential by Zetasizer nanosystem analysis and transmission electron microscopy (TEM) on carbon coated TEM copper grids by TEM respectively. Drug loading efficiency of LvN was calculated using UV-visible spectroscopy by standard curve of pure LvN. Antibacterial efficacy of Au-BRN-LvN-NPs and pure LvN was determined by evaluating minimum inhibitory concentration (MIC) against and . Two peaks were observed in Au-BRN-LvN-NPs spectrum one at 307 nm and other at 526 nm while one peak in BRN capped Au-NPs at 522 nm during UV spectroscopy suggesting red shift. The drug loading efficiency of LvN was found to be 84.8 ± 2.41 %. The diameter of Au-BRN-LvN-NPs and BRN capped Au-NPs were found to be (58.65 ± 2 nm, 38.11 ± 2 nm), zeta potential (-9.01 mV, -13.8 mV) and surface morphology (~13.2 nm, 11.4 nm) respectively. The MICs against and were found to be (0.128 µg/mL, 1.10 µg/mL) for Au-BRN-LvN-NPs and (0.547 µg/mL, 1.96 µg/mL) for pure LvN. The results suggested that BRN capped Au-NPs can be used as effective drug delivery carriers of the antibiotic LvN. The Au-BRN-LvN-NPs exhibited enhanced antibacterial activity compared to pure LvN alone. (Graphical abstract see Figure 1(Fig. 1)).

摘要

开发菠萝蛋白酶包覆的金纳米颗粒(BRN包覆的Au-NPs)作为抗生素左氧氟沙星(LvN)的有效药物递送载体,并评估其生物共轭形式与纯LvN相比的抗菌潜力。通过 方法合成BRN包覆的Au-NPs,并使用1-乙基-3-(3-二甲基氨基丙基)-碳二亚胺作为活化剂将其与LvN生物共轭,形成Au-BRN-LvN-NPs。分别通过动态光散射分析表征其平均粒径,通过Zetasizer纳米系统分析表征其zeta电位,并通过透射电子显微镜(TEM)在碳包覆的TEM铜网上进行TEM表征。通过纯LvN的标准曲线,利用紫外可见光谱法计算LvN的载药效率。通过评估对 和 的最低抑菌浓度(MIC)来确定Au-BRN-LvN-NPs和纯LvN的抗菌效果。在紫外光谱中,Au-BRN-LvN-NPs光谱中观察到两个峰,一个在307nm,另一个在526nm,而BRN包覆的Au-NPs在522nm处有一个峰,表明发生了红移。发现LvN的载药效率为84.8±2.41%。发现Au-BRN-LvN-NPs和BRN包覆的Au-NPs的直径分别为(58.65±2nm,38.11±2nm),zeta电位分别为(-9.01mV,-13.8mV),表面形态分别为(~13.2nm,11.4nm)。发现Au-BRN-LvN-NPs对 和 的MIC分别为(0.128μg/mL,1.10μg/mL),纯LvN的MIC分别为(0.547μg/mL,1.96μg/mL)。结果表明,BRN包覆的Au-NPs可作为抗生素LvN的有效药物递送载体。与单独的纯LvN相比,Au-BRN-LvN-NPs表现出增强的抗菌活性。(图形摘要见图1(图1))。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f3f5/5318683/db7d40fa97d0/EXCLI-15-772-g-001.jpg

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