Osmari Bárbara Felin, Giuliani Laura Minussi, Reolon Jéssica Brandão, Rigo Graziela Vargas, Tasca Tiana, Cruz Letícia
Laboratório de Tecnologia Farmacêutica, Programa de Pós-Graduação em Ciências Farmacêuticas, Universidade Federal de Santa Maria, Santa Maria, RS, Brazil.
Grupo de Pesquisa em Tricomonas, GPTrico(,) Laboratório de Pesquisa em Parasitologia, Faculdade de Farmácia, Universidade Federal do Rio Grande do Sul, Porto Alegre, RS, Brazil.
Eur J Pharm Sci. 2020 Aug 1;151:105379. doi: 10.1016/j.ejps.2020.105379. Epub 2020 May 27.
Trichomonas vaginalis infection is the STI most common worldwide. Indole-3-carbinol (I3C) is a phytochemical presenting promising biological activities. In this study, design, formulation, and evaluation of a vaginal hydrogel containing I3C-loaded nanocapsules for the treatment of trichomoniasis have been investigated. Nanocapsules of Eudragit® RS100 and rosehip oil containing I3C (NC-I3C) were prepared by interfacial deposition of preformed polymer method. In vitro evaluations showed that free I3C (IC50 = 3.36 µg/mL) was able to reduce the trophozoites viability at higher concentrations (3.13 and 6.25 µg/mL), while nanoencapsulation (IC50 = 2.09 µg/mL) reduced the viability at all concentrations evaluated. Comparing free and nanoencapsulated I3C, we observe that nanoencapsulation improved anti-T. vaginalis activity. In order to obtain a formulation for vaginal administration, hydrogels (HG-NC-I3C) were prepared by thickening the NC-I3C with gellan gum. HG-NC-I3C presented particle size below 195 nm, low polydispersity index (<0.2), I3C content = 0.50 ± 0.01 mg/g, pH = 7.05, non-Newtonian pseudoplastic flow behavior and exhibited mucoadhesion to cow's vaginal mucosa. Evaluation of irritation potential by chorioallantoic membrane method indicated that the formulations are considered non-irritating. Besides that, permeation through the cow's vaginal mucosa showed that nanoencapsulation promoted I3C controlled release. This way, the developed HG-NC-I3C can be considered a promising approach for trichomoniasis treatment through vaginal administration.
阴道毛滴虫感染是全球最常见的性传播感染。吲哚 - 3 - 甲醇(I3C)是一种具有潜在生物活性的植物化学物质。在本研究中,对含载有I3C的纳米胶囊的阴道水凝胶进行了设计、配方制备及治疗滴虫病的评估研究。采用预制聚合物界面沉积法制备了含I3C的Eudragit® RS100和玫瑰果油纳米胶囊(NC - I3C)。体外评估表明,游离I3C(IC50 = 3.36 µg/mL)在较高浓度(3.13和6.25 µg/mL)时能够降低滋养体活力,而纳米包封(IC50 = 2.09 µg/mL)在所有评估浓度下均能降低其活力。比较游离I3C和纳米包封的I3C,我们发现纳米包封提高了抗阴道毛滴虫活性。为了获得用于阴道给药的制剂,用结冷胶增稠NC - I3C制备了水凝胶(HG - NC - I3C)。HG - NC - I3C的粒径低于195 nm,多分散指数低(<0.2),I3C含量 = 0.50 ± 0.01 mg/g,pH = 7.05,具有非牛顿假塑性流动行为,并且对牛阴道黏膜表现出黏膜粘附性。通过绒毛尿囊膜法评估刺激潜力表明该制剂无刺激性。此外,通过牛阴道黏膜的渗透显示纳米包封促进了I3C的控释。因此,所开发的HG - NC - I3C可被认为是一种通过阴道给药治疗滴虫病的有前景的方法。