载有埃布斯硒啉的纳米乳剂对小鼠阴道念珠菌病模型的抗真菌活性评价。

Evaluation of the antifungal activity of an ebselen-loaded nanoemulsion in a mouse model of vulvovaginal candidiasis.

机构信息

Department of Pharmaceutical Sciences, St. John's University, Queens, Jamaica, NY, USA.

出版信息

Nanomedicine. 2021 Oct;37:102428. doi: 10.1016/j.nano.2021.102428. Epub 2021 Jul 1.

DOI:10.1016/j.nano.2021.102428

Abstract

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 ~562-fold compared to control (infected, untreated animals). Taken together, EB nanoemulsion proved to be an effective and promising antifungal agent.

摘要

外阴阴道念珠菌病（VVC），由白念珠菌引起，是一种常见的女性感染病，影响生活质量。标准抗真菌药物（如氟康唑、伊曲康唑）通常是抑菌或因耐药性而失效，表明迫切需要建立新的抗真菌药物储备。为了解决这个问题，我们测试了有机硒化合物 ebselen（EB）在 VVC 小鼠模型中具有抗真菌疗效的假设。EB 是一种水溶性差的药物，DMSO 作为载体，在体内给药时可能具有细胞毒性作用。开发了载有 ebselen 的自微乳前药（EB-SNEP），并进行了体外特性研究，然后在 VVC 小鼠模型中进行了测试。用 EB-SNEP（12.5mg/kg）进行的体内研究表明，与对照组（感染、未治疗的动物）相比，感染显著减少了约 562 倍。综上所述，EB 纳米乳剂被证明是一种有效且有前途的抗真菌药物。