DSPE-PEG-cRGD 修饰脂质体在靶向递送OC-2 shRNA中的应用研究

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

作者：刘春燕，赵文丽，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**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*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*组织中OC-2的表达，产生明显的**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*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。

译文：

Cationic liposome delivery of interfering RNA (shRNA) plays an important role in tumor therapy. A cyclic arginine glycine aspartate (cRGD) modified cationic liposome (cRGD-CL) was designed for targeting ONECUT2 (OC-2) shRNA (pshOC-2) to breast cancer cells. The characterization analysis of cationic liposomes showed that the prepared cRGD-CL/pshOC-2 liposome complex had uniform particle size (150 ± 1.02 nm), moderate zeta potential (19.8 ± 0.249 mV), and an encapsulation efficiency of up to 96%. The results of flow cytometry analysis showed that the introduction of cRGD can significantly promote liposome targeting of tumor cells. In MCF-7 cells, pshOC-2 can downregulate the expression of OC-2, leading to cell apoptosis, impaired scratch repair, migration, and colony formation. The Bcl xL and Bcl-2 signaling pathways are inhibited, while the Bax and Cleaved Caspase-3 signaling pathways are upregulated. In MCF-7 xenograft tumor mice, intravenous injection of cRGD-CL/pshOC-2 liposome complex can effectively reduce the expression of OC-2 in tumor tissue and produce significant anti-tumor effects, suggesting that this liposome complex may penetrate deep into the tumor through receptor-mediated phagocytic transport. The results show that cationic liposomes (cRGD-CL) is an effective OC-2 shRNA delivery system and may become an effective candidate drug for breast cancer treatment.

西安齐岳生物提供相关产品：

DSPE-PEG-Tetrazine

DSPE-PEG-TMS

DSPE-PEG-TPP

DSPE-PEG-Transferrin 

DSPE-PEG-VE, MW:2000

DSPE-PEG-β-cyclodextrin

DSPE-PEG-Ald

DSPE-PEG-Dethiobiotin

DSPE-PEG-VS

DSPE-PEG-cRGD

DSPE-PEG-KRWWKWWRR

DSPE-PEG-TAT

DSPE-PEG-CTT2

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