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Synthesis and evaluation of polymeric micelle containing piperacillin/tazobactam for enhanced antibacterial activity.
Drug Delivery ( IF 6.5 ) Pub Date : 2019-12-01 , DOI: 10.1080/10717544.2019.1693708
Milani Morteza 1, 2 , Salehi Roya 2, 3 , Hamishehkar Hamed 3 , Zarebkohan Amir 2 , Akbarzadeh Abolfazl 2
Affiliation  

Infections caused by multidrug-resistant bacteria such as P. aeruginosa are important therapeutic complications. Piperacillin/Tazobactam is considered a safe antimicrobial agent. But we should not ignore the prevalence of resistant strains to this drug. In this work, a new polymeric micelle composed of Piperacillin/Tazobactam-loaded Poly (ethylene glycol) methyl ether-block-poly (lactide-co-glycolide) (PLGA-PEG) was developed to improve the antimicrobial performance of P/T. The SEM and TEM studies of PLGA-PEG micelle showed, semi-spherical morphology with a mean diameter of below 30 nm. Zeta potential results indicated that the surface charge of PLGA-PEG micelle was -2.98 mV, while after encapsulation of P/T, the surface charge decreases to -4.13 mV. Clinical strains of P. aeruginosa were isolated and their resistance pattern against different antibiotics was evaluated. The MIC of free and P/T -Loaded PLGA-PEG micelles was determined. Also, the effect of free or P/T micelle against minimal biofilm eradication concentration and motility inhibition was evaluated. The bacterial isolates were resistant to most common antibiotics. The MIC of the free drug form and micelle form ranged from 4 to 512 µg/ml and 2 to 256 µg/ml, respectively. Generally, micelle showed more effective antibiofilm activities, inhibition of bacterial motility and reducing the MIC than that free drug form.

中文翻译:

含有哌拉西林/他唑巴坦的聚合物胶束的合成和评价,具有增强的抗菌活性。

由铜绿假单胞菌等多药耐药细菌引起的感染是重要的治疗并发症。哌拉西林/他唑巴坦被认为是安全的抗菌剂。但是,我们不应忽视这种药物耐药株的流行。在这项工作中,开发了一种新的聚合物胶束,该胶束由载有哌拉西林/他唑巴坦的聚(乙二醇)甲基醚嵌段聚(丙交酯-乙交酯)(PLGA-PEG)组成,以提高P / T的抗菌性能。PLGA-PEG胶束的SEM和TEM研究显示平均直径低于30 nm的半球形形态。Zeta电位结果表明,PLGA-PEG胶束的表面电荷为-2.98mV,而P / T包封后,表面电荷降低至-4.13mV。P.的临床菌株 分离铜绿假单胞菌并评估其对不同抗生素的抗药性。测定了游离的和P / T负载的PLGA-PEG胶束的MIC。此外,评估了游离或P / T胶束对最小生物膜清除浓度和运动抑制的影响。细菌分离株对大多数常见抗生素具有抗性。游离药物形式和胶束形式的MIC分别为4至512 µg / ml和2至256 µg / ml。通常,与游离药物相比,胶束显示出更有效的抗生物膜活性,抑制细菌运动并降低MIC。细菌分离株对大多数常见抗生素具有抗性。游离药物形式和胶束形式的MIC分别为4至512 µg / ml和2至256 µg / ml。通常,与游离药物相比,胶束显示出更有效的抗生物膜活性,抑制细菌运动并降低MIC。细菌分离株对大多数常见抗生素具有抗性。游离药物形式和胶束形式的MIC分别为4至512 µg / ml和2至256 µg / ml。通常,与游离药物相比,胶束显示出更有效的抗生物膜活性,抑制细菌运动并降低MIC。
更新日期:2019-12-01
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