Purpose

Infectious diseases caused by Candida sp. have high drug resistance due to the uncontrolled use of antibiotics. Among the natural products, ursolic acid (UA), a triterpene, has been increasing interest due to its antimicrobial effects. However, the physicochemical properties of UA, such as its low aqueous solubility, lead to failure of therapeutic application. Because of this, drug release systems, such as liquid crystals (LCs), can improve solubilization and increase the therapeutic efficacy of many drugs.

Methods

In this work, we evaluated the antifungal potential of UA and loaded into LC precursor system against Candida sp. The system was composed of oleic acid (30%), polysorbate 80 (60%), and purified water (10%). Polarized light microscopy, rheological assays, and simulated vaginal fluid (SVF) simulations were performed. Cytotoxicity assay was evaluated against L-929 cells (murine fibroblast), and antifungal evaluation was performed by microplate microdilution method against Candida albicans, Candida glabrata, Candida krusei, Candida parapsilosis, and Candida tropicalis.

Results

The system showed acceptable parameters for UA incorporation, such as adhesiveness, texture, and flow behaviors, compatible to vaginal administration. Free UA showed no antifungal activity; however, after incorporation into LCs, it was observed against C. albicans, C. glabrata, C. tropicalis, and C. parapsilosis (MIC values around 500 μg/mL and 3.9 μg/cell viability assays showed moderate cytotoxicity [halo diameter 1.00 ± 0.156]).

Conclusion

In conclusion, the results corroborate in the materials field as a possible alternative in the treatment of infectious diseases by Candida species and the systems showed potential promising for enhancing AU antifungal performance with the application on vulvovaginitis.

中文翻译：

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乌索酸在液晶体系中的结合提高了对念珠菌的抗真菌活性

目的

由念珠菌引起的传染病。由于不加控制地使用抗生素而具有很高的耐药性。在天然产物中，乌三酸（UA）（一种三萜）由于其抗菌作用而引起了越来越多的关注。然而，UA的物理化学性质，例如其低的水溶性，导致治疗应用的失败。因此，药物释放系统（例如液晶（LC））可以改善溶解度并提高许多药物的治疗功效。

方法

在这项工作中，我们评估了UA的抗真菌潜力，并将其加载到针对念珠菌的LC前体系统中。该系统由油酸（30％），聚山梨酯80（60％）和纯净水（10％）组成。进行了偏光显微镜，流变学测定和模拟阴道液（SVF）模拟。细胞毒性测定对L-929细胞（鼠成纤维细胞）来评价，并且通过微稀释法对进行抗真菌评价白色念珠菌，光滑念珠菌，克柔念珠菌，近平滑念珠菌和热带假丝酵母。

结果

该系统显示出与阴道给药相容的UA掺入的可接受参数，例如粘附性，质地和流动行为。游离UA无抗真菌活性。但是，将其掺入LC后，可观察到白色念珠菌，光滑念珠菌，热带念珠菌和副念珠菌（MIC值分别约为500μg/ mL和3.9μg/细胞，活力测定显示中等程度的细胞毒性[卤直径1.00± 0.156]）。

结论

总之，该结果在材料领域得到了证实，可作为念珠菌属感染性疾病治疗的一种可能选择，并且该系统显示出在外阴阴道炎中的应用有望增强AU抗真菌性能。