Chemistry Department, Faculty of Science, Tanta University, Tanta 31527, Egypt.
Chemistry Department, Faculty of Science, Tanta University, Tanta 31527, Egypt.
Int J Biol Macromol. 2018 Jul 15;114:717-727. doi: 10.1016/j.ijbiomac.2018.03.050. Epub 2018 Mar 13.
Norfloxacin (NOR), a well-known antibacterial agent is also known to have potential antitumor activity. In this study, NOR was immobilized into poly(3-hydroxybutyrate/polyethylene glycol‑nickel oxide (PHB/PEG-NiO) nanocomposites using different NiO contents. The NiO nanoparticles were prepared by sol-gel method and the nanocomposites were prepared by solution cast films. Physicochemical features of nanocomposites were monitored by XRD, FTIR, SEM, TEM and TGA. PHB/PEG-5%NiO nanocomposites showed high NOR loading efficiency (60%) and a long-sustained release in comparison with other carriers. The studies on the adsorption of NOR onto PHB/PEG-NiO nanocomposite revealed that the adsorption process obeyed second order kinetic and Temkin isotherm was applicable to describe the adsorption process. The mechanism of release was studied by using different kinetic equations. The loaded nanocomposites (NOR@PHB/PEG-NiO) showed effective antimicrobial activity towards gram-positive (Staphylococcus aureus), and gram-negative bacteria (E.coli and Klebsiella pneumonia). The in vitro cytotoxicity was conducted on four human cancer cell lines viz., liver Hepatocellular carcinoma, colon cancer cell, prostate cancer cell, and breast adenocarcinoma from human and one normal human amnion cell line using MTT assay. Cytotoxicity results demonstrated that NOR@PHB/PEG-NiO significantly reduced cell viability than free NOR. NOR@ PHB/PEG-NiO has about 2.5-fold more cytotoxicity as compared with free drug with a lack of cytotoxicity against normal cells.
诺氟沙星（NOR）是一种众所周知的抗菌剂，也具有潜在的抗肿瘤活性。在这项研究中，NOR 通过不同的 NiO 含量被固定到聚（3-羟基丁酸酯/聚乙二醇-氧化镍（PHB/PEG-NiO）纳米复合材料中。NiO 纳米粒子通过溶胶-凝胶法制备，纳米复合材料通过溶液浇铸薄膜制备。纳米复合材料的物理化学性质通过 XRD、FTIR、SEM、TEM 和 TGA 进行监测。与其他载体相比，PHB/PEG-5%NiO 纳米复合材料具有高 NOR 负载效率（60%）和长时间持续释放。NOR 吸附到 PHB/PEG-NiO 纳米复合材料上的研究表明，吸附过程遵循二级动力学，Temkin 等温线适用于描述吸附过程。通过使用不同的动力学方程研究了释放机制。负载的纳米复合材料（NOR@PHB/PEG-NiO）对革兰氏阳性（金黄色葡萄球菌）和革兰氏阴性菌（大肠杆菌和肺炎克雷伯菌）表现出有效的抗菌活性。体外细胞毒性实验在四种人类癌细胞系（肝癌、结肠癌、前列腺癌和乳腺癌）和一种正常人羊膜细胞系上进行，采用 MTT 法进行。细胞毒性结果表明，NOR@PHB/PEG-NiO 显著降低了细胞活力，比游离 NOR 降低了 2.5 倍。与游离药物相比，NOR@ PHB/PEG-NiO 的细胞毒性约高 2.5 倍，对正常细胞没有细胞毒性。
