DSPE-PEG-cRGD 修饰策略在shRNA递送脂质体中的应用-UDP糖丨MOF丨金属有机框架丨聚集诱导发光丨荧光标记推荐西安齐岳生物

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DSPE-PEG-cRGD 修饰策略在shRNA递送脂质体中的应用

发布时间：2025-06-27 作者：kx 分享到：

DSPE-PEG-cRGD 修饰策略在shRNA递送脂质体中的应用

文献：DSPE-PEG-cRGD修饰阳离子脂质体的制备及其对乳腺癌的*肿瘤作用

链接：https://www.mdpi.com/1999-4923/14/10/2157

作者：刘春燕，赵文丽，奥西德，张立刚，孙华敏，陈曦和邓宁

摘要：

阳离子脂质体递送干扰RNA（shRNA）在肿瘤*中发挥着重要作用。设计了环状精氨酸-甘氨酸-天冬氨酸（cRGD）修饰的阳离子脂质体（cRGD-CL），用于将ONECUT2（OC-2）shRNA（pshOC-2）靶向递送至乳腺癌细胞。阳离子脂质体的表征分析表明，制备的cRGD-CL/pshOC-2脂质体复合物粒径均一（150±1.02 nm），zeta电位适中（19.8±0.249 mV），包封率高达96%。流式细胞仪检测结果表明，cRGD的引入可显著促进脂质体靶向肿瘤细胞。在MCF-7细胞中，pshOC-2能够下调OC-2的表达，导致细胞凋亡、细胞划痕修复受阻、迁移和集落形成受阻，其中Bcl-xL和Bcl-2信号通路被抑制，Bax和Cleaved Caspase-3信号通路被上调。在MCF-7异种移植瘤小鼠中，静脉注射cRGD-CL/pshOC-2脂质体复合物可有效降低肿瘤组织中OC-2的表达，产生明显的*肿瘤作用，提示该脂质体复合物可能通过受体介导的胞吞转运作用深入肿瘤内部。结果表明，阳离子脂质体（cRGD-CL）是一种有效的OC-2 shRNA递送系统，可能成为乳腺癌*的有效候选药物。

Abstract

Cationic liposome delivery of interfering RNA (shRNA) plays an important role in tumor therapy. The cyclic Arg-Gly-Asp (cRGD) modified cationic liposomes (cRGD-CL) were designed for targeted delivery of ONECUT2 (OC-2) shRNA (pshOC-2) to breast cancer cells. The characterization analysis of cationic liposome showed that the prepared cRGD-CL/pshOC-2 lipoplexes had uniform particle size (150 ± 1.02 nm), moderate zeta potential (19.8 ± 0.249 mV) and high encapsulation efficiency (up to 96%). The results of flow cytometer showed that the introduction of cRGD could significantly promote the liposomes targeting tumor cells. In MCF-7 cells, the pshOC-2 could down-regulate expression of OC-2 and result in cell apoptosis, inhibition of the wound healing, migration and cell colony formation, in which the signal pathways of Bcl-xL, Bcl-2 were inhibited and the signal pathways of Bax and Cleaved Caspase-3 were promoted. In MCF-7 xenograft mice, intravenous administration of cRGD-CL/pshOC-2 lipoplexes could effectively reduce the expression of OC-2 in tumors and result in apparently antitumor effects, which suggested that the lipoplexes might be deeply penetrated into tumor through receptor-mediated transcytosis. The results revealed that the cationic liposome (cRGD-CL) was an effective delivery system for OC-2 shRNA, which might be an effective therapeutic candidate for breast cancer.

DSPE-PEG-cRGD