de Abreu Letícia Coli Louvisse, Todaro Valerio, Sathler Plinio Cunha, da Silva Luiz Cláudio Rodrigues Pereira, do Carmo Flávia Almada, Costa Cleonice Marques, Toma Helena Keiko, Castro Helena Carla, Rodrigues Carlos Rangel, de Sousa Valeria Pereira, Cabral Lucio Mendes
Universidade Federal do Rio de Janeiro, LabTIF, Faculdade de Farmácia, Ilha do Fundão, CEP 21941-902, Rio de Janeiro, RJ, Brazil.
Universidade Federal do Rio de Janeiro, LACMAC, Faculdade de Farmácia, Ilha do Fundão, CEP 21941-902, Rio de Janeiro, RJ, Brazil.
AAPS PharmSciTech. 2016 Dec;17(6):1421-1427. doi: 10.1208/s12249-016-0477-3. Epub 2016 Jan 25.
The aim of this work was the development and characterization of nisin-loaded nanoparticles and the evaluation of its potential antifungal activity. Candidiasis is a fungal infection caused by Candida sp. considered as one of the major public health problem currently. The discovery of antifungal agents that present a reduced or null resistance of Candida sp. and the development of more efficient drug release mechanisms are necessary for the improvement of candidiasis treatment. Nisin, a bacteriocin commercially available for more than 50 years, exhibits antibacterial action in food products with potential antifungal activity. Among several alternatives used to modulate antifungal activity of bacteriocins, polymeric nanoparticles have received great attention due to an effective drug release control and reduction of therapeutic dose, besides the minimization of adverse effects by the preferential accumulation in specific tissues. The nisin nanoparticles were prepared by double emulsification and solvent evaporation methods. Nanoparticles were characterized by dynamic light scattering, zeta potential, Fourier transform infrared, X-ray diffraction, differential scanning calorimetry, and scanning electron microscopy. Antifungal activity was accessed by pour plate method and cell counting using Candida albicans strains. The in vitro release profile and in vitro permeation studies were performed using dialysis bag method and pig vaginal mucosa in Franz diffusion cell, respectively. The results revealed nisin nanoparticles (300 nm) with spherical shape and high loading efficiency (93.88 ± 3.26%). In vitro test results suggest a promising application of these nanosystems as a prophylactic agent in recurrent vulvovaginal candidiasis and other gynecological diseases.
这项工作的目的是开发和表征负载乳链菌肽的纳米颗粒,并评估其潜在的抗真菌活性。念珠菌病是由念珠菌属引起的真菌感染,被认为是当前主要的公共卫生问题之一。发现对念珠菌属耐药性降低或无耐药性的抗真菌剂以及开发更有效的药物释放机制对于改善念珠菌病治疗是必要的。乳链菌肽是一种已上市50多年的细菌素,在食品中具有抗菌作用,并有潜在的抗真菌活性。在用于调节细菌素抗真菌活性的几种替代方法中,聚合物纳米颗粒因其能有效控制药物释放、降低治疗剂量,以及通过在特定组织中的优先积累使副作用最小化而备受关注。通过复乳法和溶剂蒸发法制备了乳链菌肽纳米颗粒。通过动态光散射、zeta电位、傅里叶变换红外光谱、X射线衍射、差示扫描量热法和扫描电子显微镜对纳米颗粒进行了表征。采用倾注平板法和使用白色念珠菌菌株进行细胞计数来评估抗真菌活性。分别使用透析袋法和Franz扩散池中猪阴道黏膜进行体外释放曲线和体外渗透研究。结果显示乳链菌肽纳米颗粒(300nm)呈球形,负载效率高(93.88±3.26%)。体外测试结果表明,这些纳米系统有望作为预防复发性外阴阴道念珠菌病和其他妇科疾病的药物。