载有埃斯硒林的生物聚合体纳米胶囊的局部递药：药物再利用增强抗真菌活性。
Topical delivery of ebselen encapsulated in biopolymeric nanocapsules: drug repurposing enhanced antifungal activity.
机构信息
Department of Lipids & Liposomes, Faculty of Biotechnology, University of Wroclaw, Joliot-Curie 14a, 50-383 Wroclaw, Poland.
Department of Medicine, Section of Infectious Diseases, 5225 Microbial Sciences Building, 1550 Linden Dr, University of Wisconsin-Madison, Madison, WI 53706, USA.
出版信息
Nanomedicine (Lond). 2018 May;13(10):1139-1155. doi: 10.2217/nnm-2017-0337. Epub 2018 Jun 6.
AIM
Ebselen (Eb) is an example of a repurposed drug with poor aqueous solubility which requires sophisticated delivery system such as nanoencapsulation in nanocapsules for topical application.
MATERIALS & METHODS: Eb-nanocapsules were examined for morphology, activity against Candida spp., cytotoxicity and skin permeation.
RESULTS
Eb-nanocapsules were active against skin-infecting Candida tropicalis, Candida albicans and Candida parapsilosis yeasts (minimal inhibitory concentration values were about 4-, 2- and 1.25-times lower vs free Eb, respectively) and able to suppress induced lipid oxidation in the oil/water emulsion. Moreover, demonstrated minimal toxicity in normal human dermal fibroblast cell line, whereas ex vivo skin permeation studies showed no transdermal passage and strong interactions with stratum corneum.
CONCLUSION
Eb-nanocapsules represent a promising, safe and complementary alternative to the treatment of cutaneous candidiasis.
目的
依布硒啉（Eb）是一种已被重新定位的药物，水溶性较差，需要复杂的输送系统，如纳米胶囊中的纳米封装，以用于局部应用。
材料与方法
研究了 Eb-纳米胶囊的形态、对念珠菌属的活性、细胞毒性和皮肤渗透。
结果
Eb-纳米胶囊对皮肤感染的热带念珠菌、白色念珠菌和近平滑念珠菌酵母菌具有活性（最小抑菌浓度值分别比游离 Eb 低约 4 倍、2 倍和 1.25 倍），并能抑制油/水乳液中诱导的脂质氧化。此外，在正常的人真皮成纤维细胞系中表现出最小的毒性，而体外皮肤渗透研究表明没有经皮传递，并且与角质层有强烈的相互作用。
结论
Eb-纳米胶囊为治疗皮肤念珠菌病提供了一种有前途的、安全的、互补的替代方法。
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