Pica Monica, Messere Nicla, Felicetti Tommaso, Sabatini Stefano, Pietrella Donatella, Nocchetti Morena
Dipartimento di Scienze Farmaceutiche, Università di Perugia, Via del Liceo, 1, 06123 Perugia, Italy.
Dipartimento di Medicina, Università di Perugia, Piazzale Gambuli, 1, 06132 Perugia, Italy.
Materials (Basel). 2021 Feb 1;14(3):670. doi: 10.3390/ma14030670.
Polymeric composites, where bioactive species are immobilized on inorganic nanostructured matrix, have received considerable attention as surfaces able to reduce bacterial adherence, colonization, and biofilm formation in implanted medical devices. In this work, potent in-house NorA efflux pump inhibitors (EPIs), belonging to the 2-phenylquinoline class, were immobilized on nanometric alpha-zirconium phosphate (ZrP) taking into advantage of acid-base or intercalation reactions. The ZrP/EPI were used as filler of poly(lactide--glycolic acid) (PLGA) to obtain film composites with a homogeneous distribution of the ZrP/EPI fillers. As reference, PLGA films loaded with ZrP intercalated with thioridazine (TZ), that is recognized as both a NorA and biofilm inhibitor, and with the antibiotic ciprofloxacin (CPX) were prepared. Composite films were characterized by X-ray diffraction, scanning electron microscopy, and thermogravimetric analysis. The ability of the composite films, containing ZrP/EPI, to inhibit biofilm formation was tested on ATCC 29213 and ATCC 12228, and it was compared with that of the composite loaded with ZrP/TZ. Finally, the antibacterial activity of CPX intercalated in ZrP was evaluated when used in combination with ZrP/EPI in the PLGA films.
生物活性物质固定在无机纳米结构基质上的聚合物复合材料，作为能够减少植入式医疗设备中细菌粘附、定植和生物膜形成的表面，受到了广泛关注。在这项工作中，利用酸碱或插层反应，将属于2-苯基喹啉类的强效内部诺氟沙星外排泵抑制剂（EPIs）固定在纳米磷酸锆（ZrP）上。ZrP/EPI用作聚乳酸-乙醇酸共聚物（PLGA）的填料，以获得ZrP/EPI填料均匀分布的薄膜复合材料。作为参考，制备了负载有插入硫利达嗪（TZ）（被认为是诺氟沙星和生物膜抑制剂）的ZrP以及抗生素环丙沙星（CPX）的PLGA薄膜。通过X射线衍射、扫描电子显微镜和热重分析对复合薄膜进行了表征。测试了含有ZrP/EPI的复合薄膜对ATCC 29213和ATCC 12228抑制生物膜形成的能力，并与负载ZrP/TZ的复合材料进行了比较。最后，评估了PLGA薄膜中ZrP插层的CPX与ZrP/EPI联合使用时的抗菌活性。
