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
Curr Mol Pharmacol. 2020;13(3):245-250. doi: 10.2174/1874467212666190821142721.
Niclosamide is an established anti-helminthic drug, which has recently been shown to inhibit the growth of various cancer cells. To exploit the potential anti-tumor activity of this drug for systemic use, the problem of low aqueous solubility should be addressed. The present study tested the in vivo anti-tumor effects of a recently developed nanoliposomal preparation of niclosamide in an experimental model of colon carcinoma.
The cytotoxicity of nanoliposomal niclosamide on CT26 colon carcinoma cells was evaluated using the MTT test. Inhibition of tumor growth was investigated in BALB/c mice bearing CT26 colon carcinoma cells. The animals were randomly divided into 4 groups including: 1) untreated control, 2) liposomal doxorubicin (15 mg/kg; single intravenous dose), 3) liposomal niclosamide (1 mg/kg/twice a week; intravenously for 4 weeks), and 4) free niclosamide (1 mg/kg/twice a week; intravenously for 4 weeks). To study therapeutic efficacy, tumor size and survival were monitored in 2-day intervals for 40 days.
In vitro results indicated that nanoliposomal and free niclosamide could exert cytotoxic effects with IC50 values of 4.5 and 2.5 μM, respectively. According to in vivo studies, nanoliposomal niclosamide showed a higher growth inhibitory activity against CT26 colon carcinoma cells compared with free niclosamide as revealed by delayed tumor growth and prolongation of survival.
Nnaoliposomal encapsulation enhanced anti-tumor properties of niclosamide in an experimental model of colon carcinoma.
尼氯硝唑是一种已被证实的抗蠕虫药物，最近有研究表明它可以抑制多种癌细胞的生长。为了开发这种药物的全身应用潜力，应该解决其水溶性低的问题。本研究在结直肠癌的实验模型中测试了最近开发的尼氯硝唑纳米脂质体制剂的体内抗肿瘤作用。
采用 MTT 试验评估纳米脂质体尼氯硝唑对 CT26 结肠癌细胞的细胞毒性。在荷 CT26 结肠癌细胞的 BALB/c 小鼠中研究了肿瘤生长抑制作用。动物随机分为 4 组：1）未处理对照组；2）脂质体多柔比星（15mg/kg；单次静脉注射）；3）脂质体尼氯硝唑（1mg/kg/每周 2 次；静脉注射 4 周）；4）游离尼氯硝唑（1mg/kg/每周 2 次；静脉注射 4 周）。为了研究治疗效果，在 40 天内每隔 2 天监测肿瘤大小和存活情况。
体外结果表明，纳米脂质体和游离尼氯硝唑均可发挥细胞毒性作用，IC50 值分别为 4.5 和 2.5μM。根据体内研究结果，与游离尼氯硝唑相比，纳米脂质体尼氯硝唑对 CT26 结肠癌细胞的生长抑制活性更高，表现为肿瘤生长延迟和存活时间延长。
纳米脂质体包封增强了尼氯硝唑在结直肠癌实验模型中的抗肿瘤特性。
