Development and Antibacterial Investigation of Linezolid-Loaded SPIONs and HPLC Method Development for Quantitative Analysis of Linezolid.

IF 1.7 4区 农林科学 Q3 CHEMISTRY, ANALYTICAL
Musarrat Husain Warsi, Sharmistha Mohapatra, Mohammed Asfer, Mohammad Yusuf, Abuzer Ali, Mohammad Akhlaquer Rahman, Amena Ali, Abdul Qadir, Gaurav K Jain
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Abstract

Background: Linezolid (LNZ) is extremely prone to resistance. The development of resistance to LNZ should be taken into consideration when selecting this drug as a therapeutic option. It is well established that reactive oxygen species (ROS) generated by iron oxide nanoparticles (MNPs) could kill the infecting bacteria. So, we hypothesized the synergistic antibacterial effect of iron oxide nanoparticles and LNZ.

Objective: To study the release and antibacterial effects of LNZ-loaded superparamagnetic iron oxide nanoparticles (SPIONs) on Staphylococcus aureus and Streptococcus pneumoniae.

Method: Ferrofluid containing SPIONs was synthesized via chemical co-precipitation method and stabilized by sodium lauryl sulphate (SLS). SPIONs were then loaded with LNZ and characterized for particle size, FT-IR, XRD, and entrapment efficiency. Further antibacterial activity of SPIONs and LNZ-loaded SPIONs was investigated. For the in vitro release findings, HPLC analytical method development and validation were performed.

Results: Isolation of LNZ was accomplished on a C-18 column with methanol-TBHS (tetra butyl ammonium hydrogen sulphate, 50:50, v/v). The eluate was monitored at 247 nm with a retention time of 4.175 min. The MNP's DLS measurement revealed monodispersed particles with an average size of 16.81 ± 1.07 nm and PDI 0.176 ± 0.012. In optimized formulation, 25 ± 1.75% (w/w) of the drug was found to be entrapped. XRD revealed uniform coating of oleic acid covering the entire magnetic particles' surface with no change in its crystallinity. An effective antimicrobial activity was observed at the lowered dose of drug.

Conclusions: A robust HPLC method was developed to quantify the LNZ in MNPs, and outcomes showed that the reduced dose of LNZ incorporated in SPIONs was able to show similar activity as the marketed product.

Highlights: Successfully reduction of the dose of LNZ was established with the aid of biocompatible MNPs to attain the equivalent antibacterial activity.

利奈唑胺负载SPIONs的开发与抗菌研究及利奈唑胺定量分析方法的建立。
背景:利奈唑胺(LNZ)极易产生耐药性。在选择这种药物作为治疗方案时,应考虑到对LNZ的耐药性的发展。由氧化铁纳米颗粒(MNPs)产生的活性氧(ROS)可以杀死感染细菌。因此,我们假设氧化铁纳米颗粒与LNZ具有协同抑菌作用。目的:研究负载lnz的超顺磁性氧化铁纳米颗粒(SPIONs)对金黄色葡萄球菌和肺炎链球菌的释放及抑菌作用。方法:采用化学共沉淀法合成含SPIONs的铁磁流体,并用十二烷基硫酸钠(SLS)稳定。然后用LNZ负载SPIONs,并对其粒径、FT-IR、XRD和包封效率进行表征。进一步研究了SPIONs和负载lnz的SPIONs的抑菌活性。对其体外释放结果进行了HPLC分析方法的建立和验证。结果:在C-18色谱柱上甲醇- tbhs(硫酸四丁基氢铵,50:50,v/v)分离得到LNZ。洗脱液在247 nm处监测,保留时间为4.175 min。MNP的DLS测量显示单分散颗粒的平均尺寸为16.81±1.07 nm, PDI为0.176±0.012。在优化后的配方中,药物的包封率为25±1.75% (w/w)。XRD分析表明,磁性颗粒表面均匀覆盖油酸层,结晶度没有变化。在较低剂量下观察到有效的抗菌活性。结论:建立了高效液相色谱定量MNPs中LNZ的方法,结果表明,SPIONs中LNZ的减少剂量能够显示出与上市产品相似的活性。重点:在生物相容性MNPs的帮助下,成功地减少了LNZ的剂量,达到了等效的抗菌活性。
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来源期刊
Journal of AOAC International
Journal of AOAC International 医学-分析化学
CiteScore
3.10
自引率
12.50%
发文量
144
审稿时长
2.7 months
期刊介绍: The Journal of AOAC INTERNATIONAL publishes the latest in basic and applied research in analytical sciences related to foods, drugs, agriculture, the environment, and more. The Journal is the method researchers'' forum for exchanging information and keeping informed of new technology and techniques pertinent to regulatory agencies and regulated industries.
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