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3-Methoxyazetidin-2-one Functionalized CuO–CB Microfibrils: A Drug Formulation with Controlled Release and Enhanced Synergistic Antibacterial Activities
ACS Applied Bio Materials ( IF 4.6 ) Pub Date : 2023-04-19 , DOI: 10.1021/acsabm.3c00064
Anjali Vijeata 1 , Ganga Ram Chaudhary 1 , Aman Bhalla 1 , Savita Chaudhary 1
Affiliation  

trans-1-(4′-Methoxyphenyl)-3-methoxy-4-phenyl 3-methoxyazetidin-2-one (or 3-methoxyazetidin-2-one) is one of the important β-lactam derivatives with an ample range of bacterial activities yet few restrictions. To enhance the competency of the chosen 3-methoxyazetidin-2-one, microfibrils composed of copper oxide (CuO) and filter scraps of cigarette butts (CB) were chosen in the current work for developing a potential release formulation. The preparation of CuO-CB microfibrils required a simple reflux technique and a subsequent calcination treatment. The loading of 3-methoxyazetidin-2-one was processed via controlled magnetic stirring followed by centrifugation with microfibrils of CuO-CB. To confirm the loading efficiency, the 3-methoxyazetidin-2-one@CuO-CB complex was analyzed by scanning electron microscopy, transmission electron microscopy, and infrared spectroscopy. Compared to the CuO nanoparticles, the release profile of CuO-CB microfibrils indicates only 32% of the drug release in the first 1 h at pH 7.4. As a model organism, E. coli has been utilized for in vitro drug release dynamic studies. Based on the observed drug release data, it was found that the prepared formulation evades premature drug release and triggers the on-demand release of drug inside bacterial cells. The controlled drug release by 3-methoxyazetidin-2-one@CuO-CB microfibrils over a period of 12 h further ascertained the excellent bactericide delivery mechanism to combat deadly bacterial resistance. Indeed, this study provides a strategy to combat antimicrobial resistance and eradicate bacterial disease via nanotherapeutics.

中文翻译:

3-Methoxyazetidin-2-one 功能化 CuO-CB 微纤维:一种具有控释和增强协同抗菌活性的药物制剂

反式-1-(4'-Methoxyphenyl)-3-methoxy-4-phenyl 3-methoxyazetidin-2-one (or 3-methoxyazetidin-2-one) 是重要的β-内酰胺衍生物之一,具有广泛的细菌活性但限制很少。为了提高所选 3-methoxyazetidin-2-one 的能力,在当前的工作中选择了由氧化铜 (CuO) 和烟头过滤屑 (CB) 组成的微纤维来开发潜在的释放配方。CuO-CB 微纤维的制备需要简单的回流技术和随后的煅烧处理。3-methoxyazetidin-2-one 的负载通过受控磁力搅拌处理,然后用 CuO-CB 微纤维离心。为了确认负载效率,通过扫描电子显微镜、透射电子显微镜、和红外光谱。与 CuO 纳米颗粒相比,CuO-CB 微纤维的释放曲线表明在 pH 7.4 的前 1 小时内只有 32% 的药物释放。作为模式生物,大肠杆菌已被用于体外药物释放动态研究。根据观察到的药物释放数据,发现所制备的制剂避免了过早的药物释放,并触发了药物在细菌细胞内的按需释放。3-methoxyazetidin-2-one@CuO-CB 微纤维在 12 小时内的控制药物释放进一步确定了对抗致命细菌耐药性的优异杀菌剂递送机制。事实上,这项研究提供了一种通过纳米疗法对抗抗菌素耐药性和根除细菌性疾病的策略。
更新日期:2023-04-19
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