a Department of Pharmaceutical Sciences , University of Calabria , Arcavacata di Rende , Cosenza , Italy and.
b Virology and Microbiology Service of "Annunziata" Hospital , Cosenza , Italy.
Drug Deliv. 2016;23(3):1047-56. doi: 10.3109/10717544.2014.932862. Epub 2014 Jul 9.
The present article reports the preparation, characterization and performance evaluation of solid lipid nanoparticles (SLNs) based on polyoxyethylene-40 stearate (PEG-40 stearate) for the administration of antifungal agents such as ketoconazole and clotrimazole. These nanoparticles could be useful in the treatment of vaginal infections sustained by Candida albicans. In particular, PEG-40 stearate was made to react with acryloyl chloride in order to introduce an easily polymerizable moiety for the creation of a second shell and to ensure a slow drug release. In addition, the differences on the release profiles between PEG-40 stearate-based nanoparticles, PEG-40 stearate acrylate based and polymerized ones, were analyzed under conditions, simulating the typical environment of Candida albicans infection. Then, the antifungal activity of nanoparticles was also evaluated in terms of minimal inhibitory concentration. Moreover, the nanoparticles were submitted to in vitro studies for evaluating the drug permeability at the site of action. Results indicated that the obtained particles are potentially useful for the treatment of vaginal infections sustained by Candida albicans.
本文报道了基于聚氧乙烯 40 硬脂酸酯（PEG-40 硬脂酸酯）的固体脂质纳米粒（SLNs）的制备、表征和性能评价，用于管理抗真菌药物，如酮康唑和克霉唑。这些纳米粒在治疗由白色念珠菌引起的阴道感染方面可能有用。特别是，PEG-40 硬脂酸酯与丙烯酰氯反应，以引入易于聚合的部分，用于形成第二壳，并确保药物缓慢释放。此外，在模拟白色念珠菌感染典型环境的条件下，分析了基于 PEG-40 硬脂酸酯的纳米粒、基于 PEG-40 硬脂酸酯丙烯酸酯的纳米粒和聚合纳米粒之间的释放曲线差异。然后，根据最小抑菌浓度评估了纳米粒的抗真菌活性。此外，还对纳米粒进行了体外研究，以评估药物在作用部位的渗透性。结果表明，所得到的颗粒在治疗由白色念珠菌引起的阴道感染方面具有潜在的应用价值。
