Novel Hybrid Formulations Based on Thiourea Derivatives and Core@Shell Fe₃O₄@C18 Nanostructures for the Development of Antifungal Strategies

基于硫脲衍生物和核@壳 Fe₃O₄@C18 纳米结构的新型混合配方,用于开发抗真菌策略

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作者:Carmen Limban, Alexandru Vasile Missir, Miron Teodor Caproiu, Alexandru Mihai Grumezescu, Mariana Carmen Chifiriuc, Coralia Bleotu, Luminita Marutescu, Marius Toma Papacocea, Diana Camelia Nuta1

Abstract

The continuously increasing global impact of fungal infections is requiring the rapid development of novel antifungal agents. Due to their multiple pharmacological activities, thiourea derivatives represent privileged candidates for shaping new drugs. We report here the preparation, physico-chemical characterization and bioevaluation of hybrid nanosystems based on new 2-((4-chlorophenoxy)methyl)-N-(substituted phenylcarbamo-thioyl)benzamides and Fe&sub3;O&sub4;@C18 core@shell nanoparticles. The new benzamides were prepared by an efficient method, then their structure was confirmed by spectral studies and elemental analysis and they were further loaded on Fe&sub3;O&sub4;@C18 nanostructures. Both the obtained benzamides and the resulting hybrid nanosystems were tested for their efficiency against planktonic and adherent fungal cells, as well as for their in vitro biocompatibility, using mesenchymal cells. The antibiofilm activity of the obtained benzamides was dependent on the position and nature of substituents, demonstrating that structure modulation could be a very useful approach to enhance their antimicrobial properties. The hybrid nanosystems have shown an increased efficiency in preventing the development of Candida albicans (C. albicans) biofilms and moreover, they exhibited a good biocompatibility, suggesting that Fe&sub3;O&sub4;@C18core@shell nanoparticles could represent promising nanocarriers for antifungal substances, paving the way to the development of novel effective strategies with prophylactic and therapeutic value for fighting biofilm associated C. albicans infections.

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