Xiaoli Mao1,2, Junjie Liu1, Zhirong Gong1, He Zhang1, Ying Lu1,2, Hao Zou1, Yuan Yu1, Yan Chen1, Zhiguo Sun1, Wei Li3, Bohua Li3, Jie Gao1, Yanqiang Zhong1,2. 1. Department of Pharmaceutical Sciences, School of Pharmacy, Second Military Medical University, 325 Guohe Road, Shanghai 200433, China. 2. School of Pharmacy, Fujian University of Traditional Chinese Medicine, Fujian, China. 3. International Joint Cancer Institute, Second Military Medical University, 800 Xiangyin Road, Shanghai 200433, China.
Abstract
AIMS: To develop novel iRGD (internalizing Arg-Gly-Asp peptide)-conjugated DSPE-PEG2000 nanomicelles (M-SAL-iRGD) for delivery of salinomycin to both liver cancer cells and cancer stem cells (CSCs). MATERIALS & METHODS: The characterization, antitumor activity and mechanism of action of M-SAL-iRGD were evaluated. RESULTS & CONCLUSION: M-SAL-iRGD possessed a small size of around 10 nm, and drug encapsulation efficacy higher than 90%. M-SAL-iRGD showed significantly increased cytotoxic effect toward both nontargeted M-SAL (salinomycin-loaded DSPE-PEG2000 nanomicelles) and salinomycin in both liver cancer cells and CSCs. The tissue distribution and antitumor assays in mice bearing liver cancer xenograft confirmed the superior penetration tumor efficacy and antitumor activity of M-SAL-iRGD. M-SAL-iRGD represent a potential effective nanomedicine against liver cancer.
AIMS: To develop novel iRGD (internalizing Arg-Gly-Asp peptide)-conjugated DSPE-PEG2000 nanomicelles (M-SAL-iRGD) for delivery of salinomycin to both liver cancer cells and cancer stem cells (CSCs). MATERIALS & METHODS: The characterization, antitumor activity and mechanism of action of M-SAL-iRGD were evaluated. RESULTS & CONCLUSION: M-SAL-iRGD possessed a small size of around 10 nm, and drug encapsulation efficacy higher than 90%. M-SAL-iRGD showed significantly increased cytotoxic effect toward both nontargeted M-SAL (salinomycin-loaded DSPE-PEG2000 nanomicelles) and salinomycin in both liver cancer cells and CSCs. The tissue distribution and antitumor assays in mice bearing liver cancer xenograft confirmed the superior penetration tumor efficacy and antitumor activity of M-SAL-iRGD. M-SAL-iRGD represent a potential effective nanomedicine against liver cancer.
Entities:
Keywords:
cancer nanotechnology; cancer stem cells; iRGD; liver cancer; micelles
Authors: Paola Pellegrini; Matheus Dyczynski; Francesca Vittoria Sbrana; Maria Karlgren; Maria Buoncervello; Maria Hägg-Olofsson; Ran Ma; Johan Hartman; Svetlana Bajalica-Lagercrantz; Dan Grander; Pedram Kharaziha; Angelo De Milito Journal: Oncotarget Date: 2016-06-14