Cholesterol-tuned liposomal membrane rigidity directs tumor penetration and anti-tumor effect
文献类型：期刊论文
| 作者 | Wu Hangyi2; Yu Miaorong1; Miao Yunqiu1; He Shufang1; Dai Zhuo1; Song Wenyi1; Liu Yuan1; Song Sha1; Ahmad Ejaj1; Wang Dongkai2 |
| 刊名 | Acta Pharmaceutica Sinica B
 |
| 出版日期 | 2019 |
| 卷号 | 9期号:4页码:858-870 |
| 关键词 | Therapeutics. Pharmacology RM1-950 |
| ISSN号 | 2211-3835 |
| 其他题名 | Cholesterol-tuned liposomal membrane rigidity directs tumor penetration and anti-tumor effect |
| 英文摘要 | Recently, liposomes have been widely used in cancer therapeutics, but their anti-tumor effects are suboptimal due to limited tumor penetration. To solve this problem, researchers have made significant efforts to optimize liposomal diameters and potentials, but little attention has been paid to liposomal membrane rigidity. Herein, we sought to demonstrate the effects of cholesterol-tuned liposomal membrane rigidity on tumor penetration and anti-tumor effects. In this study, liposomes composed of hydrogenated soybean phospholipids (HSPC), 1,2-distearoyl-sn-glycero-3-phosphoethanolamine-N-methoxy(polyethylene glycol)-2000 (DSPE-PEG2000) and different concentrations of cholesterol were prepared. It was revealed that liposomal membrane rigidity decreased with the addition of cholesterol. Moderate cholesterol content conferred excellent diffusivity to liposomes in simulated diffusion medium, while excessive cholesterol limited the diffusion process. We concluded that the differences of the diffusion rates likely stemmed from the alterations in liposomal membrane rigidity, with moderate rigidity leading to improved diffusion. Next, the in vitro tumor penetration and the in vivo anti-tumor effects were analyzed. The results showed that liposomes with moderate rigidity gained excellent tumor penetration and enhanced anti-tumor effects. These findings illustrate a feasible and effective way to improve tumor penetration and therapeutic efficacy of liposomes by changing the cholesterol content, and highlight the importance of liposomal membrane rigidity. KEY WORDS: Cholesterol, Liposomal membrane rigidity, Tumor penetration, Anti-tumor effects |
| 资助项目 | [National Natural Science Foundation of China] ; [Science and Technology Innovation Action Plan for Basic Research of Shanghai 2014 (China)] ; [Shanghai Sailing Program 2017 (China)] ; [K.C.Wong Education Foundation (China)] |
| 语种 | 英语 |
| CSCD记录号 | CSCD:6552418 |
| 源URL | [http://ir.imr.ac.cn/handle/321006/89804]  |
| 专题 | 金属研究所_中国科学院金属研究所 |
| 作者单位 | 1.中国科学院 2.中国科学院金属研究所 |
| 推荐引用方式 GB/T 7714 | Wu Hangyi,Yu Miaorong,Miao Yunqiu,et al. Cholesterol-tuned liposomal membrane rigidity directs tumor penetration and anti-tumor effect[J]. Acta Pharmaceutica Sinica B,2019,9(4):858-870. |
| APA | Wu Hangyi.,Yu Miaorong.,Miao Yunqiu.,He Shufang.,Dai Zhuo.,...&Gan Yong.(2019).Cholesterol-tuned liposomal membrane rigidity directs tumor penetration and anti-tumor effect.Acta Pharmaceutica Sinica B,9(4),858-870. |
| MLA | Wu Hangyi,et al."Cholesterol-tuned liposomal membrane rigidity directs tumor penetration and anti-tumor effect".Acta Pharmaceutica Sinica B 9.4(2019):858-870. |
入库方式： OAI收割
来源：金属研究所
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