Nanotechnology Research Center, Pharmaceutical Technology Institute, Mashhad University of Medical Sciences, Mashhad, Iran.
Biotechnology Research Center, Pharmaceutical Technology Institute, Mashhad University of Medical Sciences, Mashhad, Iran.
Anticancer Agents Med Chem. 2019;19(13):1618-1626. doi: 10.2174/1871520619666190705120011.
Niclosamide is an FDA-approved and old anti-helminthic drug used to treat parasitic infections. Recent studies have shown that niclosamide has broad anti-tumor effects relevant to the treatment of cancer. However, this drug has a low aqueous solubility hindering its systemic use. Herein, we report the preparation and characterization of niclosamide nanoliposomes and their anti-tumor effects.
Nanoliposomes were prepared using thin-film method and the drug was encapsulated with a remote loading method. The nanoliposomes were investigated by the observation of morphology, analysis of particle size and zeta potential. Additionally, qualitative and quantitative analyses were performed using HPLC. We assessed the cytotoxicity of the nanoliposomal niclosamide on B16F10 melanoma cells. Inhibition of tumor growth was investigated in C57BL/6 mice bearing B16F0 melanoma cancer.
Analytical results indicated that the nanoliposomal system is a homogeneous and stable colloidal dispersion of niclosamide particles. Atomic force microscopy images and particle size analysis revealed that all niclosamide particles had a spherical shape with a diameter of approximately 108nm. According to and studies, nanoliposomal niclosamide exhibited a better anti-tumor activity against B16F10 melanoma tumor compared with free niclosamide.
Nanoliposomal encapsulation enhanced the aqueous solubility of niclosamide and improved its anti-tumor properties.
尼氯硝唑是一种获得美国食品和药物管理局批准的、用于治疗寄生虫感染的老的驱虫药。最近的研究表明，尼氯硝唑具有广泛的抗肿瘤作用，与癌症的治疗有关。然而，这种药物的水溶解度低，阻碍了其系统应用。本文报道了尼氯硝唑纳米脂质体的制备和表征及其抗肿瘤作用。
采用薄膜法制备纳米脂质体，采用远程加载法包封药物。通过观察形态、分析粒径和zeta 电位对纳米脂质体进行研究。此外，还采用高效液相色谱法进行定性和定量分析。我们评估了尼氯硝唑纳米脂质体对 B16F10 黑色素瘤细胞的细胞毒性。在携带 B16F0 黑色素瘤癌症的 C57BL/6 小鼠中研究了肿瘤生长的抑制作用。
分析结果表明，纳米脂质体系统是一种均匀稳定的尼氯硝唑颗粒胶体分散体。原子力显微镜图像和粒径分析表明，所有尼氯硝唑颗粒均呈球形，直径约为 108nm。根据 和 研究，与游离尼氯硝唑相比，纳米脂质体包封的尼氯硝唑对 B16F10 黑色素瘤肿瘤具有更好的抗肿瘤活性。
纳米脂质体包封提高了尼氯硝唑的水溶解度，并改善了其抗肿瘤特性。
