Evaluation of the antifungal activity of an ebselen-loaded nanoemulsion in a mouse model of vulvovaginal candidiasis
Evaluation of the antifungal activity of an ebselen-loaded nanoemulsion in a mouse model of vulvovaginal candidiasis
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DOI：
10.1016/j.nano.2021.102428
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发表时间：
2021-07-28
影响因子：
5.4
通讯作者：
Billack, Blase
中科院分区：
文献类型：
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作者：
Menon, Suvidha;Vartak, Richa;Billack, Blase
外阴阴道念珠菌病 (VVC) 由白色念珠菌引起，是女性常见的感染，影响她们的生活质量。标准抗真菌药物（例如氟康唑、伊曲康唑）通常具有抑制真菌的作用，或者由于耐药性而变得无效，这表明迫切需要建立新型抗真菌药物库。为了解决这个问题，我们测试了有机硒化合物依布硒啉 (EB) 在 VVC 小鼠模型中具有抗真菌功效的假设。 EB 是一种水溶性较差的药物，而 DMSO 作为载体在体内给药时有可能表现出细胞毒性作用。开发了 EB 负载自纳米乳化预浓缩物 (EB-SNEP)，进行了体外表征，并在 VVC 小鼠模型中进行了测试。使用 EB-SNEP (12.5 mg/kg) 进行的体内研究表明，与对照（受感染的未治疗动物）相比，感染显着减少了约 562 倍。综上所述，EB纳米乳被证明是一种有效且有前途的抗真菌剂。 (C) 2021 Elsevier Inc. 保留所有权利。
Vulvovaginal candidiasis (VVC), caused by Candida albicans, is a common infection in women affecting their quality of life. Standard antifungal drugs (e.g., fluconazole, itraconazole) are typically fungistatic or rendered ineffective due to drug resistance indicating an urgent need to build an arsenal of novel antifungal agents. To surmount this issue, we tested the hypothesis that the organoselenium compound ebselen (EB) possesses antifungal efficacy in a mouse model of VVC. EB is a poorly water-soluble drug and DMSO as a vehicle has the potential to exhibit cytotoxic effects when administered in vivo. EB loaded self-nanoemulsifying preconcentrate (EB-SNEP) was developed, characterized in vitro, and tested in a mouse model of VVC. In vivo studies carried out with EB-SNEP (12.5 mg/kg) showed a remarkable decrease in infection by similar to 562-fold compared to control (infected, untreated animals). Taken together, EB nanoemulsion proved to be an effective and promising antifungal agent. (C) 2021 Elsevier Inc. All rights reserved.