Teaima Mahmoud H, Elasaly Mohamed K, Omar Samia A, El-Nabarawi Mohamed A, Shoueir Kamel R
Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Cairo, Egypt.
Department of Pharmaceutics, Faculty of Pharmacy, Ahram Canadian University, Giza, Egypt.
Saudi Pharm J. 2020 Jul;28(7):859-868. doi: 10.1016/j.jsps.2020.06.005. Epub 2020 Jun 18.
To obtain a healthy human being with beneficial microflora against different pathogenic infections, classical antibiotics with nanosized biomaterials were used to inhibit the growth of bacterium by their potent synergistic effect. Hence, this study planned to load an oxazolidinone antibiotic named linezolid (LD) onto functionalized chitosan (CN) with 3, 5- dinitrosalyslic acid (DA) via microwave synthesis without harsh condition. The exploring synergistic effect of linezolid (LD) with CN/DA controllable nanostructure was compact efflux-mediated methicillin-resistant (MRSA) burden and other selected bactericide Gram-positive ( Gram-negative (), and . The obtained results showed that LD was incorporated into both the internal and external surface of the aggregated CN/DA nanosystem with an average diameter of 150 nm ± 4 hints of the drug loading. Owing to the nature of functionalized CN, the release efficiency attains 98.4% within 100 min. The designed LD@CN/DA exhibited inhibition zone 54 mm, 59 mm, 69 mm, 54 mm, 57 mm, and 24 mm against the tested microbes respectively rather than individual LD. The major target of the current research is achieved by using LD@CN/DA as a nanoantibiotic system that has exceptional consistently active against multi-resistant pathogens, in between MRSA which resist LD. Also, cell viability was performed even after three days of direct cell culture on the surface of the designed nanoantibiotic. The mechanism of microbial inhibition was correlated and rationalized to different charges and the presence of oxygen species against microbial infections. Our findings provide a deep explanation about nanostructured antibiotics design with enhanced potentially pathogen-specific activity.
为了获得具有有益微生物群以抵御不同致病感染的健康个体，将经典抗生素与纳米级生物材料结合使用，通过其强大的协同作用来抑制细菌生长。因此，本研究计划通过微波合成，在无苛刻条件下，将一种名为利奈唑胺（LD）的恶唑烷酮类抗生素负载到用3,5 - 二硝基水杨酸（DA）功能化的壳聚糖（CN）上。探索利奈唑胺（LD）与CN/DA可控纳米结构的协同效应，对耐甲氧西林金黄色葡萄球菌（MRSA）负担以及其他选定的革兰氏阳性菌（革兰氏阴性菌（）和）具有显著作用。所得结果表明，LD被纳入聚集的CN/DA纳米系统的内表面和外表面，其平均直径为150 nm ± 4，载药量为。由于功能化CN的性质,释放效率在100分钟内达到98.4%。所设计的LD@CN/DA对受试微生物的抑菌圈分别为54 mm、59 mm、69 mm、54 mm、57 mm和24 mm，优于单独的LD。本研究的主要目标是通过使用LD@CN/DA作为纳米抗生素系统来实现的，该系统对多重耐药病原体具有卓越且持续的活性，介于对LD耐药的MRSA之间。此外，即使在设计的纳米抗生素表面直接进行细胞培养三天后，细胞活力仍得以保持。微生物抑制机制与不同电荷以及对抗微生物感染的氧物种的存在相关并得到合理解释。我们的研究结果为具有增强的潜在病原体特异性活性的纳米结构抗生素设计提供了深入解释。
