Synthesis and evaluation of polymeric micelle containing piperacillin/tazobactam for enhanced antibacterial activity

Drug Delivery

Zarebkohan Amir¹  Akbarzadeh Abolfazl¹  Hamishehkar Hamed²  Salehi Roya³  Milani Morteza⁴ 

[1] Department of Medical Nanotechnology, Faculty of Advanced Medical Sciences, Tabriz University of Medical Sciences, Tabriz, Ira;Drug Applied Research Center, Tabriz University of Medical Sciences, Tabriz, Iran;Drug Applied Research Center, Tabriz University of Medical Sciences, Tabriz, Iran;Department of Medical Nanotechnology, Faculty of Advanced Medical Sciences, Tabriz University of Medical Sciences, Tabriz, Ira;Infectious and Tropical Diseases Research Center, Tabriz University of Medical Sciences, Tabriz, Iran;Department of Medical Nanotechnology, Faculty of Advanced Medical Sciences, Tabriz University of Medical Sciences, Tabriz, Ira;

关键词: P. aeruginosa;    piperacillin/tazobactam;    polymeric micelle;    antibiotic resistance;   

DOI  :  10.1080/10717544.2019.1693708

来源: publisher

【 摘 要 】

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.

【 授权许可】

CC BY