Ahmed Saleh A, Nur Hasan Md, Bagchi Damayanti, Altass Hatem M, Morad Moataz, Althagafi Ismail I, Hameed Ahmed M, Sayqal Ali, Khder Abd El Rahman S, Asghar Basim H, Katouah Hanadi A, Pal Samir Kumar
Department of Chemistry, Faculty of Applied Science, Umm Al-Qura University, 21955 Makkah, Saudi Arabia.
Chemistry Department, Faculty of Science, Assiut University, 71516 Assiut, Egypt.
R Soc Open Sci. 2020 Dec 2;7(12):200959. doi: 10.1098/rsos.200959. eCollection 2020 Dec.
The drug resistance of bacteria is a significant threat to human civilization while the action of antibiotics against drug-resistant bacteria is severely limited owing to the hydrophobic nature of drug molecules, which unquestionably inhibit its permanency for clinical applications. The antibacterial action of nanomaterials offers major modalities to combat drug resistance of bacteria. The current work reports the use of nano-metal-organic frameworks encapsulating drug molecules to enhance its antibacterial activity against model drug-resistant bacteria and biofilm of the bacteria. We have attached rifampicin (RF), a well-documented antituberculosis drug with tremendous pharmacological significance, into the pore surface of zeolitic imidazolate framework 8 (ZIF8) by a simple synthetic procedure. The synthesized ZIF8 has been characterized using the X-ray diffraction (XRD) method before and after drug encapsulation. The electron microscopic strategies such as scanning electron microscope and transmission electron microscope methods were performed to characterize the binding between ZIF8 and RF. We have also performed picosecond-resolved fluorescence spectroscopy to validate the formation of the ZIF8-RF nanohybrids (NHs). The drug release profile experiment demonstrates that ZIF8-RF depicts pH-responsive drug delivery and is ideal for targeting bacterial disease corresponding to its inherent acidic nature. Most remarkably, ZIF8-RF gives enhanced antibacterial activity against methicillin-resistant bacteria and also prompts entire damage of structurally robust bacterial biofilms. Overall, the present study depicts a detailed physical insight for manufactured antibiotic-encapsulated NHs presenting tremendous antimicrobial activity that can be beneficial for manifold practical applications.
细菌的耐药性对人类文明构成了重大威胁，而由于药物分子的疏水性，抗生素对耐药菌的作用受到严重限制，这无疑阻碍了其在临床应用中的持久性。纳米材料的抗菌作用为对抗细菌耐药性提供了主要方式。目前的工作报道了使用封装药物分子的纳米金属有机框架来增强其对模型耐药菌及其生物膜的抗菌活性。我们通过一种简单的合成方法将利福平（RF），一种具有巨大药理学意义的著名抗结核药物，附着到沸石咪唑酯框架8（ZIF8）的孔表面。在药物封装前后，使用X射线衍射（XRD）方法对合成的ZIF8进行了表征。采用扫描电子显微镜和透射电子显微镜等电子显微镜技术来表征ZIF8与RF之间的结合。我们还进行了皮秒分辨荧光光谱分析，以验证ZIF8-RF纳米杂化物（NHs）的形成。药物释放曲线实验表明，ZIF8-RF呈现出pH响应性药物递送，并且由于其固有的酸性性质，对于靶向细菌性疾病是理想的。最显著的是，ZIF8-RF对耐甲氧西林细菌具有增强的抗菌活性，并且还促使结构坚固的细菌生物膜完全受损。总体而言，本研究对制造的具有巨大抗菌活性的抗生素封装纳米杂化物进行了详细的物理洞察，这对多种实际应用可能是有益的。
