Salahuddin Nehal, Gaber Mohamed, Mousa Maie, Abdelwahab Mohamed A
Chemistry Department, Faculty of Science, Tanta University Tanta 31527 Egypt
RSC Adv. 2020 Sep 17;10(56):34046-34058. doi: 10.1039/d0ra04784h. eCollection 2020 Sep 10.
Sustained release dosage forms enable prolonged and continuous release of a drug in the gastrointestinal tract for medication characterized by a short half lifetime. In this study, the effect of blending polyamine on poly(3-hydroxybutyrate) (PHB) as a carrier for norfloxacin (NF) was studied. The prepared blend was mixed with different amounts of NiO nanoparticles and characterized using FTIR analysis, X-ray diffraction analysis, thermogravimetric analysis, dynamic light scattering, transmission electron microscopy and scanning electron microscopy. It was found that the drug released from the nanocomposite has a slow rate in comparison with NiO, PHB, and PHB/polyamine blend. The highest ratio of NiO content to the matrix (highest NF loading), leads to a slower rate of drug release. The release from the nanocomposites showed a faster rate at pH = 2 than that at pH = 7.4. The mechanisms of NF adsorption and release were studied on PHB/polyamine-3% NiO nanocomposite. In addition, the antimicrobial efficacy of nanocomposites loaded with the drug was determined and compared with the free drug. Inclusion of NiO into PHB/polyamine showed a higher efficacy against and than the free NF. Moreover, the cytotoxicity of PHB/polyamine-3% NiO against HePG-2 cells was investigated and compared with PHB and PHB/polyamine loaded with the drug. The most efficient IC was found for NF@PHB/polyamine-3% NiO (29.67 μg mL). No effect on cell proliferation against the normal human cell line (WISH) was observed and IC was detected to be 44.95 and 70 μg mL for NiO nanoparticles and the PHB/polyamine-3% NiO nanocomposite, respectively indicating a selectivity of action towards tumor cells coupled with a lack of cytotoxicity towards normal cells.
缓释剂型能够使药物在胃肠道中长时间持续释放,适用于半衰期短的药物。在本研究中,研究了将多胺与聚(3-羟基丁酸酯)(PHB)共混作为诺氟沙星(NF)载体的效果。将制备的共混物与不同量的NiO纳米颗粒混合,并通过傅里叶变换红外光谱分析、X射线衍射分析、热重分析、动态光散射、透射电子显微镜和扫描电子显微镜进行表征。结果发现,与NiO、PHB和PHB/多胺共混物相比,纳米复合材料释放药物的速率较慢。NiO含量与基质的比例最高(NF负载量最高)时,药物释放速率较慢。纳米复合材料在pH = 2时的释放速率比在pH = 7.4时更快。研究了PHB/多胺-3% NiO纳米复合材料对NF的吸附和释放机制。此外,测定了载药纳米复合材料的抗菌效果,并与游离药物进行了比较。将NiO加入PHB/多胺中对[具体菌种1]和[具体菌种2]的抗菌效果比游离NF更高。此外,研究了PHB/多胺-3% NiO对HePG-2细胞的细胞毒性,并与载药的PHB和PHB/多胺进行了比较。发现NF@PHB/多胺-3% NiO的最有效半数抑制浓度(IC)为29.67 μg/mL。未观察到对正常人细胞系(WISH)细胞增殖的影响,NiO纳米颗粒和PHB/多胺-3% NiO纳米复合材料的IC分别为44.95和70 μg/mL,表明对肿瘤细胞具有作用选择性,对正常细胞缺乏细胞毒性。