Mostafavi Mahshid, Khazaeli Payam, Sharifi Iraj, Farajzadeh Saeedeh, Sharifi Hamid, Keyhani Alireza, Parizi Maryam Hakimi, Kakooei Sina
Leishmaniasis Research Center, Kerman University of Medical Sciences, Kerman, Iran.
Department of Pharmaceutics, Faculty of Pharmacy, Kerman University of Medical Sciences, Kerman, Iran.
Korean J Parasitol. 2019 Feb;57(1):1-8. doi: 10.3347/kjp.2019.57.1.1. Epub 2019 Feb 26.
There is no effective treatment modality available against different forms of leishmaniasis. Therefore, the aim of this study was to improve the penetration and efficacy of selenium and glucantime coupled with niosomes and compared them with their simple forms alone on in vitro susceptibility assays. In this study, the niosomal formulations of selenium and in combination with glucantime were prepared. The size and morphology of the niosomal formulations were characterized and the effectivity of the new formulation was also evaluated using in vitro MTT assay, intra-macrophage model, and gene expression profile. From the results obtained, no cytotoxicity effect was observed for niosomal and simple forms of drugs, as alone or in combination. Niosomal formulations of the drugs significantly showed more inhibitory effects (P ≤ 0.001) than the simple drugs when the selectivity index was considered. The gene expression levels of Interleukin (IL-10) significantly decreased, while the level of IL-12 and metacaspase significantly increased (P ≤ 0.001). The results of the present study showed that selenium plus glucantime niosome possess a potent anti-leishmanial effect and enhanced their lethal activity as evidenced by the in vitro experiments.
目前尚无针对不同形式利什曼病的有效治疗方法。因此，本研究的目的是提高硒和葡糖胺锑钠与脂质体结合后的渗透性和疗效，并在体外药敏试验中将它们与单独的简单形式进行比较。在本研究中，制备了硒的脂质体制剂及其与葡糖胺锑钠的组合制剂。对脂质体制剂的大小和形态进行了表征，并使用体外MTT试验、巨噬细胞内模型和基因表达谱评估了新制剂的有效性。从获得的结果来看，单独或组合使用时，脂质体形式和简单形式的药物均未观察到细胞毒性作用。当考虑选择性指数时，药物的脂质体制剂比简单药物显示出更显著的抑制作用（P≤0.001）。白细胞介素（IL-10）的基因表达水平显著降低，而IL-12和metacaspase的水平显著升高（P≤0.001）。本研究结果表明，硒加葡糖胺锑钠脂质体具有强大的抗利什曼原虫作用，并增强了它们的致死活性，体外实验证明了这一点。
