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| 核黄素修饰的脂质复合纳米粒共递送CXCR4 siRNA和阿霉素治疗高转移性癌症 | |
| 引用本文： | 李锴森,王如东,彭祎玮,董达文,齐宪荣. 核黄素修饰的脂质复合纳米粒共递送CXCR4 siRNA和阿霉素治疗高转移性癌症[J]. 中国药学, 2021, 30(3): 189-205. DOI: 10.5246/jcps.2021.03.015 |
| 作者姓名： | 李锴森 王如东 彭祎玮 董达文 齐宪荣 |
| 摘 要： | 多项研究揭示SDF-1/CXCR4是与癌症转移最相关的趋化因子通路之一,因此靶向CXCR4的siRNA能够改善高转移性癌症治疗效果,尤其将其与化疗联合使用时潜力巨大.本研究中,我们构建了素修饰的脂质复合纳米粒,实现了对CXCR4 siRNA和阿霉素的共递送,用于癌症治疗.以酸性环境中可断裂的腙键,将阿霉素共价连接至聚乙... |
| 关 键 词： | 核黄素 脂质复合纳米粒 共递送 小干扰RNA 阿霉素 |
| 收稿时间： | 2020-09-05 |
Riboflavin-modified lipo-polyplexes co-delivering CXCR4 siRNA and doxorubicin for treatment of highly metastatic cancer |
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| Kaisen Li,Rudong Wang,Yiwei Peng,Dawen Dong,Xianrong Qi. Riboflavin-modified lipo-polyplexes co-delivering CXCR4 siRNA and doxorubicin for treatment of highly metastatic cancer[J]. Journal of Chinese Pharmaceutical Sciences, 2021, 30(3): 189-205. DOI: 10.5246/jcps.2021.03.015 | |
| Authors: | Kaisen Li Rudong Wang Yiwei Peng Dawen Dong Xianrong Qi |
| Abstract: | SDF-1/CXCR4 has been recognized as one of the most relevant chemokine signaling pathways to cancer metastasis, and siRNA targeting CXCR4 may provide potential improvements to treat those highly metastatic cancers, especially when combined with chemotherapy. In the present study, we constructed riboflavin-modified lipo-polyplexes to co-deliver CXCR4 siRNA and doxorubicin for cancer therapy. Doxorubicin was covalently conjugated to polyethyleneimine (PEI) with acid-cleavable hydrazine bond, and the obtained acid-sensitive conjugate was efficiently condensed with siRNA to form polyplexes, which were further coated with riboflavin-tailed lipid-membrane to prepare the lipo-polyplexes conveniently. Utilizing the fact that tumor cells overexpress riboflavin receptors, the riboflavin modification effectively enhanced uptake of lipo-polyplexes by tumor cells in a receptor-mediated manner. The riboflavin-modified lipo-polyplexes co-delivering CXCR4 siRNA and doxorubicin effectively decreased viability and invasiveness of tumor cells in vitro, and inhibited primary tumor growth and tumor metastasis in vivo. |
| Keywords: | Riboflavin Lipo-polyplexes Co-delivery SiRNA Doxorubicin |
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