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载两性霉素 B 的 Eudragit RL100 纳米粒经透明质酸包被用于治疗外阴阴道念珠菌病。

Amphotericin B-loaded Eudragit RL100 nanoparticles coated with hyaluronic acid for the treatment of vulvovaginal candidiasis.

机构信息

School of Pharmacy, Federal University of São João del-Rei, Divinópolis, Minas Gerais, Brazil.

School of Pharmacy, Federal University of Ouro Preto, Ouro Preto, Minas Gerais, Brazil.

出版信息

Carbohydr Polym. 2020 Feb 15;230:115608. doi: 10.1016/j.carbpol.2019.115608. Epub 2019 Nov 11.

Abstract

The treatment of vulvovaginal candidiasis (VVC) is based on oral and vaginal formulations which show limited effectiveness. In this study, amphotericin B-loaded Eudragit RL100 nanoparticles coated with hyaluronic acid (AMP EUD nanoparticles/HA) were developed to overcome the drawbacks of the conventional formulations. AMP EUD nanoparticles/HA were synthesized by nanoprecipitation, formulated by statistical experimental design, and characterized. AMP release from EUD nanoparticles/HA and its antifungal activity in a murine model of VVC were evaluated. Nanoparticles showed 147.6 ± 16.7 nm of diameter, 0.301 ± 0.09 of polydispersity index, - 29.9 ± 3.76 mV of zeta potential, and 87.27 % of encapsulation efficiency. They released about 81 % of AMP in 96 h; and provided the elimination of 100 % of the vaginal fungal burden in 24 h. It was suggested that the AMP EUD nanoparticles/HA penetrated into the vaginal epithelium via CD44 receptors. These AMP EUD nanoparticles/HA represent a non-conventional vaginal formulation to improve the treatment of VVC.

摘要

外阴阴道念珠菌病 (VVC) 的治疗基于口服和阴道制剂,但这些制剂的效果有限。在这项研究中,开发了负载两性霉素 B 的 Eudragit RL100 纳米粒,并用透明质酸(AMP EUD 纳米粒/HA)进行涂层,以克服传统制剂的缺点。通过纳米沉淀合成 AMP EUD 纳米粒/HA,通过统计实验设计进行配方,并进行了表征。评估了 EUD 纳米粒/HA 中 AMP 的释放及其在 VVC 小鼠模型中的抗真菌活性。纳米粒的直径为 147.6±16.7nm,多分散指数为 0.301±0.09,Zeta 电位为-29.9±3.76mV,包封效率为 87.27%。它们在 96 小时内释放了约 81%的 AMP;并在 24 小时内消除了 100%的阴道真菌负担。研究表明,AMP EUD 纳米粒/HA 通过 CD44 受体穿透阴道上皮。这些 AMP EUD 纳米粒/HA 代表了一种非传统的阴道制剂,可以改善 VVC 的治疗效果。

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