Guzel Kaya Gulcihan, Medaglia Serena, Candela-Noguera Vicente, Tormo-Mas María Ángeles, Marcos María Dolores, Aznar Elena, Deveci Huseyin, Martínez-Máñez Ramón
Department of Chemical Engineering, Konya Technical University, Ardıçlı Mah. Rauf Orbay Cad, Selçuklu, 42250 Konya, Turkey.
Instituto Interuniversitario de Investigación de Reconocimiento Molecular y Desarrollo Tecnológico, Universitat Politècnica de València, Universitat de València, Camino de Vera s/n, 46022 Valencia, Spain.
Pharmaceutics. 2020 Nov 21;12(11):1126. doi: 10.3390/pharmaceutics12111126.
In recent times, many approaches have been developed against drug resistant Gram-negative bacteria. However, low-cost high effective materials which could broaden the spectrum of antibiotics are still needed. In this study, enhancement of linezolid spectrum, normally active against Gram-positive bacteria, was aimed for Gram-negative bacteria growth inhibition. For this purpose, a silica xerogel prepared from a low-cost precursor is used as a drug carrier owing to the advantages of its mesoporous structure, suitable pore and particle size and ultralow density. The silica xerogel is loaded with linezolid and capped with ε-poly-l-lysine. The developed nano-formulation shows a marked antibacterial activity against to , and In comparison to free linezolid and ε-poly-l-lysine, the material demonstrates a synergistic effect on killing for the three tested bacteria. The results show that silica xerogels can be used as a potential drug carrier and activity enhancer. This strategy could provide the improvement of antibacterial activity spectrum of antibacterial agents like linezolid and could represent a powerful alternative to overcome antibiotic resistance in a near future.
近年来，已经开发出许多针对耐药革兰氏阴性菌的方法。然而，仍然需要能够拓宽抗生素谱的低成本高效材料。在本研究中，旨在增强利奈唑胺（通常对革兰氏阳性菌有活性）对革兰氏阴性菌生长的抑制作用。为此，由低成本前驱体制备的二氧化硅干凝胶由于其介孔结构、合适的孔径和粒径以及超低密度的优点而被用作药物载体。二氧化硅干凝胶负载有利奈唑胺并用ε-聚-L-赖氨酸封端。所开发的纳米制剂对 、 和 显示出显著的抗菌活性。与游离利奈唑胺和ε-聚-L-赖氨酸相比，该材料对三种受试细菌的杀灭具有协同作用。结果表明，二氧化硅干凝胶可作为潜在的药物载体和活性增强剂。该策略可以改善像利奈唑胺这样的抗菌剂的抗菌活性谱，并且在不久的将来可能成为克服抗生素耐药性的有力替代方法。
