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环丙沙星功能化生物陶瓷植入物的抗菌效果增强:一项计算机模拟和体外研究。

Enhanced Antibacterial Efficacy of Bioceramic Implants Functionalized with Ciprofloxacin: An In Silico and In Vitro Study.

作者信息

Văruț Renata-Maria, Rotaru Luciana Teodora, Cimpoesu Diana, Corlade Mihaela, Singer Cristina Elena, Popescu Alin Iulian Silviu, Popescu Cristina, Iulian-Nicolae Iliescu, Mocanu Adriana, Popescu Mihaela, Butoi Mihai Alexandru, Nicolaescu Oana Elena

机构信息

Research Methodology Department, Faculty of Pharmacy, University of Medicine and Pharmacy of Craiova, 200349 Craiova, Romania.

Emergency Medicine and First Aid Department, Faculty of Medicine, University of Medicine and Pharmacy of Craiova, 200349 Craiova, Romania.

出版信息

Pharmaceutics. 2024 Jul 28;16(8):998. doi: 10.3390/pharmaceutics16080998.

Abstract

This study explores the antibacterial efficacy and cytotoxicity of ciprofloxacin-functionalized bioceramic implants. We synthesized hydroxyapatite-ciprofloxacin (HACPX) composites and applied them to titanium substrates (Ti-HA-CPX), evaluating their performance in vitro against (ATCC 25923) and (ATCC 25922). Antibacterial activity was assessed using the Kirby-Bauer disc diffusion method, while cytotoxicity was tested using mesenchymal stem cells. The results demonstrated that Ti-HA-CPX exhibited superior antibacterial activity, with inhibition zones of 33.5 mm (MIC 0.5 µg/mL) for (ATCC 25923) and 27.5 mm (MIC 0.25 µg/mL) for (ATCC 25922). However, Ti-HA-CPX showed moderate cytotoxicity (80% cell viability). HACPX composites, whether chemically synthesized or mechanically mixed (HACPX), also displayed significant antibacterial activity, but with cytotoxicity ranging from low to moderate levels. Molecular docking studies confirmed strong binding affinities between ciprofloxacin and bacterial proteins, correlating with enhanced antibacterial efficacy. These findings suggest that Ti-HA-CPX composites offer a promising approach for single-stage surgical interventions in treating chronic osteomyelitis and infected fractures, balancing antibacterial effectiveness with manageable cytotoxicity.

摘要

本研究探讨了环丙沙星功能化生物陶瓷植入物的抗菌效果和细胞毒性。我们合成了羟基磷灰石 - 环丙沙星(HACPX)复合材料,并将其应用于钛基底(Ti - HA - CPX),评估它们在体外对金黄色葡萄球菌(ATCC 25923)和大肠杆菌(ATCC 25922)的性能。使用 Kirby - Bauer 纸片扩散法评估抗菌活性,同时使用间充质干细胞测试细胞毒性。结果表明,Ti - HA - CPX表现出优异的抗菌活性,对金黄色葡萄球菌(ATCC 25923)的抑菌圈为33.5毫米(MIC 0.5微克/毫升),对大肠杆菌(ATCC 25922)的抑菌圈为27.5毫米(MIC 0.25微克/毫升)。然而,Ti - HA - CPX显示出中度细胞毒性(细胞活力80%)。HACPX复合材料,无论是化学合成的还是机械混合的(HACPX),也都表现出显著的抗菌活性,但细胞毒性范围从低到中度。分子对接研究证实了环丙沙星与细菌蛋白之间有很强的结合亲和力,这与增强的抗菌效果相关。这些发现表明,Ti - HA - CPX复合材料为治疗慢性骨髓炎和感染性骨折的单阶段手术干预提供了一种有前景的方法,在抗菌效果和可控制的细胞毒性之间取得了平衡。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6b2b/11358898/b29d0e258408/pharmaceutics-16-00998-g001.jpg

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