Post-Graduate Program in Pharmaceutical Science, State University of Maringá, avenue Colombo, 5790, Maringá 87020-900, Paraná, Brazil.
Post-Graduate Program in Pharmaceutical Science, State University of Maringá, avenue Colombo, 5790, Maringá 87020-900, Paraná, Brazil.
J Mycol Med. 2020 Sep;30(3):101003. doi: 10.1016/j.mycmed.2020.101003. Epub 2020 May 24.
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.
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.
Spherical nanoparticles, with a mean diameter of 188.5nm 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.
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.
为提高酮康唑的疗效，制备了载酮康唑的聚乳酸（PLA）纳米粒，并对其进行了表征，同时检测了其对皮肤癣菌和念珠菌浮游细胞和生物膜细胞的作用。
采用纳米沉淀法制备酮康唑-PLA 纳米粒，并用动态光散射、扫描电子显微镜、透射电子显微镜和差示扫描量热法进行了表征。此外，还测定了包封酮康唑的定量和体外释放曲线。对皮肤癣菌红色毛癣菌、须癣毛癣菌和石膏样小孢子菌以及酵母白色念珠菌、都柏林念珠菌、克柔念珠菌、近平滑念珠菌和热带念珠菌进行了抗真菌药敏试验。
获得了平均直径为 188.5nm、酮康唑包封效率为 45%的球形纳米粒。载酮康唑纳米粒对所有测试真菌菌株的抗真菌活性均优于游离酮康唑。同时还抑制了酵母生物膜的形成。
酮康唑-PLA 纳米粒使酮康唑纳米粒的抗真菌活性优于游离药物，对皮肤癣菌和念珠菌属具有潜在的治疗作用。
