University of Oradea, Medicine and Pharmacy Faculty, Piata 1 Decembrie, 410028, Oradea, Romania.
Vasile Goldis" Western University of Arad, Pharmacy Faculty, 86 Liviu Rebreanu Street, 310045, Arad, Romania.
Int J Infect Dis. 2020 Dec;101:65-73. doi: 10.1016/j.ijid.2020.09.1465. Epub 2020 Oct 1.
To synthesize and characterize the inclusion complexes of fusidic acid with β - cyclodextrin, followed by the evaluation of their antimicrobial activity against pure strain (Staphylococcus aureus ATCC 25,923) and isolated Staphylococcus from clinical cases.
The desired compounds were synthesized using molar ratio of fusidic acid: β-cyclodextrin of 1:1. Synthesized compounds were analyzed by Fourier Transform Infrared Spectroscopy (FTIR), X-Ray Diffraction (XRD), Scanning Electron Microscopy (SEM), and Thermal Analysis, and the results confirmed the formation of inclusion compounds by fusidic acid with β-cyclodextrin.
Physical-chemical characterization confirmed the preparation of desired inclusion compounds, and the antimicrobial test confirmed that all compounds obtained have antimicrobial activity. Antimicrobial activity of freeze-drying complex againstS. aureus is similar with pure fusidic acid activity, being better than the cefoxitin one. Similar behavior was observed against methicillin-resistant S. aureus and S. epidermidis.
In the present work, three different inclusion complexes of fusidic acid were prepared using three different preparation methods. All inclusion complexes obtained presented good antimicrobial activity against differentS. aureus strains. Antimicrobial activity of these new prepared compounds was observed to be better than that of cefoxitin.
合成并表征游离酸与β-环糊精的包合物，然后评估它们对纯菌株（金黄色葡萄球菌 ATCC 25923）和从临床分离的金黄色葡萄球菌的抗菌活性。
采用游离酸：β-环糊精摩尔比为 1:1 的方法合成所需化合物。通过傅里叶变换红外光谱（FTIR）、X 射线衍射（XRD）、扫描电子显微镜（SEM）和热分析对合成化合物进行分析，结果证实了游离酸与β-环糊精形成包合物。
物理化学特性证实了所需包合物的制备，抗菌试验证实所有获得的化合物均具有抗菌活性。冻干复合物对金黄色葡萄球菌的抗菌活性与游离酸相似，优于头孢西丁。对耐甲氧西林金黄色葡萄球菌和表皮葡萄球菌也观察到类似的行为。
在本工作中，使用三种不同的制备方法制备了三种不同的游离酸包合物。所有获得的包合物对不同的金黄色葡萄球菌菌株均表现出良好的抗菌活性。这些新制备化合物的抗菌活性优于头孢西丁。
