Objective

In order to improve the effect of ketoconazole, poly-lactic acid (PLA) nanoparticles containing ketoconazole were prepared, characterized and tested against dermatophytes and Candida spp planktonic and biofilm cells.

Methods

The ketoconazole-PLA nanoparticles obtained by nanoprecipitation were characterized using dynamic light scattering, scanning electron microscopy, transmission electron microscopy, and differential scanning calorimetry. In addition, quantification of encapsulated ketoconazole and the in vitro release profile were determined. Antifungal susceptibility tests against dermatophytes Trichophyton rubrum, Trichophyton mentagrophytes, and Microsporum gypseum and yeasts Candida albicans, C. dubliniensis, C. krusei, C. parapsilosis, and C. tropicalis were performed.

Results

Spherical nanoparticles, with a mean diameter of 188.5 nm and an encapsulation efficiency of 45% ketoconazole, were obtained. The nanoparticles containing ketoconazole had superior antifungal activity against all tested fungi strains than free ketoconazole. Inhibition of yeast biofilm formation was also achieved.

Conclusion

Ketoconazole-PLA nanoparticles resulted in better antifungal activity of ketoconazole nanoparticles than free drug against dermatophytes and Candida species, indicating a promising tool for the development of therapeutic strategies.

中文翻译：

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酮康唑负载的聚乳酸纳米颗粒：体外抗念珠菌和皮肤真菌的特性和抗真菌功效的提高。

目的

为了提高酮康唑的作用，制备了含有酮康唑的聚乳酸（PLA）纳米颗粒，对皮肤癣菌和念珠菌浮游生物和生物膜细胞进行了表征和测试。

方法

使用动态光散射，扫描电子显微镜，透射电子显微镜和差示扫描量热法对通过纳米沉淀获得的酮康唑-PLA纳米颗粒进行了表征。另外，确定了包封的酮康唑的定量和体外释放曲线。对皮肤癣菌的抗真菌敏感性试验红色毛癣菌，须毛癣菌，和孢子gypseum和酵母菌白色念珠菌，C.都柏林，克柔念珠菌，近平滑念珠菌，和热带念珠菌进行。

结果

获得了球形纳米颗粒，其平均直径为188.5 nm，封装效率为45％酮康唑。含有酮康唑的纳米颗粒对所有测试真菌菌株的抗真菌活性均优于游离酮康唑。还实现了对酵母生物膜形成的抑制。

结论

酮康唑-PLA纳米颗粒比游离药物对皮肤癣菌和念珠菌具有更好的抗真菌活性，这为开发治疗策略提供了有希望的工具。