Wang Meiping, Xie Fangyuan, Wen Xikai, Chen Han, Zhang Hai, Liu Junjie, Zhang He, Zou Hao, Yu Yuan, Chen Yan, Sun Zhiguo, Wang Xinxia, Zhang Guoqing, Yin Chuan, Sun Duxin, Gao Jie, Jiang Beige, Zhong Yanqiang, Lu Ying
Department of Pharmaceutical Sciences, Second Military Medical University, 325 Guohe Road, Shanghai 200433, China.
Department of Pharmacy, Shanghai Eastern Hepatobiliary Surgery Hospital, 225 Changhai Road, Shanghai 200438, China.
Nanomedicine (Lond). 2017 May;12(9):1025-1042. doi: 10.2217/nnm-2016-0408. Epub 2017 Apr 25.
Salinomycin (SAL)-loaded PEG-ceramide nanomicelles (SCM) were prepared to target both liver cancer cells and cancer stem cells.
MATERIALS & METHODS: The synergistic ratio of SAL/PEG-ceramide was evaluated to prepare SCM, and the antitumor activity of SCM was examined both in vitro and in vivo.
SAL/PEG-ceramide molar ratio of 1:4 was chosen as the synergistic ratio, and SCM showed superior cytotoxic effect and increased apoptosis-inducing activity in both liver cancer cells and cancer stem cells. In vivo, SCM showed the best tumor inhibitory effect with a safety profile.
Thus, PEG-ceramide nanomicelles could serve as an effective and safe therapeutic drug carrier to deliver SAL into liver cancer, opening up the avenue of using PEG-ceramide as therapeutic drug carriers.
制备负载沙林霉素(SAL)的聚乙二醇 - 神经酰胺纳米胶束(SCM),以靶向肝癌细胞和癌症干细胞。
评估SAL/聚乙二醇 - 神经酰胺的协同比例以制备SCM,并在体外和体内检测SCM的抗肿瘤活性。
选择1:4的SAL/聚乙二醇 - 神经酰胺摩尔比作为协同比例,SCM在肝癌细胞和癌症干细胞中均显示出优异的细胞毒性作用和增强的凋亡诱导活性。在体内,SCM显示出最佳的肿瘤抑制效果且具有安全性。
因此,聚乙二醇 - 神经酰胺纳米胶束可作为一种有效且安全的治疗药物载体,将SAL递送至肝癌中,开辟了将聚乙二醇 - 神经酰胺用作治疗药物载体的途径。