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Enhancing azithromycin antibacterial activity by encapsulation in liposomes/liposomal-N-acetylcysteine formulations against resistant clinical strains of Escherichia coli
Saudi Journal of Biological Sciences ( IF 4.4 ) Pub Date : 2020-09-12 , DOI: 10.1016/j.sjbs.2020.09.012
Shokran A. Aljihani , Zeyad Alehaideb , Reem E. Alarfaj , Majed F. Alghoribi , Maaged A. Akiel , Thamer H. Alenazi , Ahmed J. Al-Fahad , Saad M. Al Tamimi , Turki M. Albakr , Abdulrahman Alshehri , Saad M. Alyahya , Alaa Eldeen B. Yassin , Majed A. Halwani

E. coli is an Enterobacteriaceae that could develop resistance to various antibiotics and become a multi-drug resistant (MDR) bacterium. Options for treating MDR E. coli are limited and the pipeline is somewhat dry when it comes to antibiotics for MDR bacteria, so we aimed to explore more options to help in treating MDR E. coli. The purpose of this study is to examine the synergistic effect of a liposomal formulations of co-encapsulated azithromycin and N-acetylcysteine against E. coli. Liposomal azithromycin (LA) and liposomal azithromycin/N-acetylcysteine (LAN) were compared to free azithromycin. A broth dilution was used to measure the MIC and MBC of both formulations. The biofilm reduction activity, thermal stability measurements, stability studies, and cell toxicity analysis were performed. LA and LAN effectively reduced the MIC of E. coli SA10 strain, to 3 μg/ml and 2.5 μg/ml respectively. LAN at 1 × MIC recorded a 93.22% effectiveness in reducing an E. coli SA10 biofilm. The LA and LAN formulations were also structurally stable to 212 ± 2 °C and 198 ± 3 °C, respectively. In biological conditions, the formulations were largely stable in PBS conditions; however, they illustrated limited stability in sputum and plasma. We conclude that the formulation presented could be a promising therapy for E. coli resistance circumstances, providing the stability conditions have been enhanced.



中文翻译:

针对抗性临床分离株中的脂质体增强阿奇霉素的抗菌活性通过封装/脂质体-N-乙酰半胱氨酸的制剂大肠杆菌

大肠杆菌是一种肠杆菌科细菌,可能对多种抗生素产生耐药性,并成为多药耐药(MDR)细菌。治疗耐多药大肠埃希氏菌的选择有限,涉及耐多药多药细菌的抗生素时,管道有些干燥,因此我们旨在探索更多选项来帮助治疗耐多药埃希氏菌。这项研究的目的是检查共包裹的阿奇霉素和N-乙酰半胱氨酸的脂质体制剂对大肠杆菌的协同作用将脂质体阿奇霉素(LA)和脂质体阿奇霉素/ N-乙酰半胱氨酸(LAN)与游离阿奇霉素进行比较。用肉汤稀释液测量两种制剂的MIC和MBC。进行了生物膜还原活性,热稳定性测量,稳定性研究和细胞毒性分析。LA和LAN有效地将大肠杆菌SA10菌株的MIC分别降低至3μg/ ml和2.5μg/ ml。MIC为1×MIC的局域网在减少大肠杆菌方面的有效性为93.22%SA10生物膜。LA和LAN配方分别在212±2°C和198±3°C下也具有结构稳定性。在生物学条件下,该制剂在PBS条件下基本稳定。然而,他们证明了痰液和血浆的稳定性有限。我们得出的结论是只要稳定性条件得到改善,所提出的制剂可能是一种针对大肠杆菌耐药情况的有前途的疗法。

更新日期:2020-10-14
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