Akbar Noor, Gul Jasra, Siddiqui Ruqaiyyah, Shah Muhammad Raza, Khan Naveed Ahmed
College of Arts and Sciences, American University of Sharjah, University City, Sharjah 26666, United Arab Emirates.
International Centre for Chemical and Biological Sciences, H.E.J. Research Institute of Chemistry, University of Karachi, Karachi 75270, Pakistan.
Antibiotics (Basel). 2021 Aug 11;10(8):964. doi: 10.3390/antibiotics10080964.
Antibiotic resistance is a major concern given the rapid emergence of multiple-drug-resistant bacteria compared to the discovery of novel antibacterials. An alternative strategy is enhancing the existing available drugs. Nanomedicine has emerged as an exciting area of research, showing promise in the enhanced development of existing antimicrobials. Herein, we synthesized nanocarriers and loaded these with available clinically approved drugs, namely Moxifloxacin and Sulfamethoxazole. Bactericidal activity against Gram-negative (, , , and ) and Gram-positive (methicillin-resistant , , and ) bacteria was investigated. To characterize the nanocarriers and their drug-loaded forms, Fourier-transform infrared spectroscopy, dynamic light scattering, and atomic force microscopy were utilized. Antibacterial assays and hemolysis assays were carried out. Moreover, lactate dehydrogenase assays were performed to determine cytotoxicity against human cells. The results depicted the successful formation of drug-nanocarrier complexes. The potent antibacterial activities of the drug-loaded nanocarriers were observed and were significantly enhanced in comparison to the drugs alone. Hemolysis and cytotoxicity assays revealed minimal or negligible cytotoxic effects against human red blood cells and human cells. Overall, metronidazole-based nanocarriers loaded with Moxifloxacin and Sulfamethoxazole showed enhanced bactericidal effects against multiple-drug-resistant bacteria compared with drugs alone, without affecting human cells. Our findings show that drug-loaded nanocarriers hold promise as potent chemotherapeutic drugs against multiple-drug-resistant bacteria.
鉴于多重耐药菌的迅速出现,与新型抗菌药物的发现相比,抗生素耐药性成为一个主要问题。一种替代策略是增强现有的可用药物。纳米医学已成为一个令人兴奋的研究领域,在增强现有抗菌药物的研发方面显示出前景。在此,我们合成了纳米载体,并将临床批准的可用药物莫西沙星和磺胺甲恶唑装载到这些纳米载体中。研究了其对革兰氏阴性菌(大肠杆菌、肺炎克雷伯菌、铜绿假单胞菌和鲍曼不动杆菌)和革兰氏阳性菌(耐甲氧西林金黄色葡萄球菌、表皮葡萄球菌和金黄色葡萄球菌)的杀菌活性。利用傅里叶变换红外光谱、动态光散射和原子力显微镜对纳米载体及其载药形式进行表征。进行了抗菌试验和溶血试验。此外,还进行了乳酸脱氢酶试验以确定对人细胞的细胞毒性。结果表明成功形成了药物 - 纳米载体复合物。观察到载药纳米载体具有强大的抗菌活性,与单独的药物相比显著增强。溶血和细胞毒性试验显示对人红细胞和人细胞的细胞毒性极小或可忽略不计。总体而言,装载莫西沙星和磺胺甲恶唑的基于甲硝唑的纳米载体与单独的药物相比,对多重耐药菌显示出增强的杀菌效果,且不影响人体细胞。我们的研究结果表明,载药纳米载体有望成为对抗多重耐药菌的有效化疗药物。