文献：Observation of antitumor mechanism of GE11-modified paclitaxel and curcumin liposomes based on cellular morphology changes

文献链接：https://link.springer.com/article/10.1186/s41120-023-00090-9

作者：Hailing Tang , Lijuan Li , Baoshan Wang

相关产品：DSPE-PEG2000-GE11

原文摘要：

Curcumin and paclitaxel are widely used as anti-tumor hydrophobic model drugs for the designation of smart tumor-targeting nanocarriers and the study of the correlation between structural characteristics of nanoparticles and in vivo therapeutic efficacy. Various signaling pathways on cell growth and proliferation have been comprehensively studied in vitro and in vivo under the action of curcumin and paclitaxel nanoparticles. In this paper, we prepared EGFR-targeted GE11 peptide-modified curcumin and paclitaxel compound liposomes (CUR-PTX@GE11-L). The tumor suppression mechanism of CUR-PTX@GE11-L is observed from the aspects of drug release behavior, changes of cell morphology, liver retention, and tumor-targeting efficiency. We hope it can provide a new vision for the rational construction of smart nanoscale drug delivery system through the observation of cytotoxic effects of CUR-PTX@GE11-L, especially on the cellular morphology change.   

DSPE-PEG2000-GE11：一种复杂的化合物。它主要由三部分组成，DSPE（1,2 - 二硬脂酰 - sn - 甘油 - 3 - 磷酸乙醇胺）是一种磷脂成分，具有亲脂性。PEG2000 表示聚乙二醇部分的分子量约为 2000Da，聚乙二醇是一种亲水性的聚合物，能够增加化合物的水溶性和生物相容性。GE11 是一种具有特定生物活性的肽段，它赋予了该化合物靶向识别等功能。基于DSPE-PEG2000-GE11的性能，复合脂质体CUR-PTX@GE11-L的合成如下：

图：机制示意

分别制备EPC、 CHOL、DSPE-PEG2000、DSPE-PEG2000- ge11、CUR、2PTX乙醇脂质储备液。根据CUR-PTX@GE11-L脂质配方制备乙醇脂质相。脂质体样品采用INano快速纳米修复器制备。所得脂质体样品以葡萄糖为水相，用旋转蒸发器除去杂质，4℃保存。CUR-PTX@GE11-L是通过两步制备的。首先，分别制备姜黄素和紫杉醇脂质体（CUR-PTX@L）、DSPE-PEG2000胶束和DSPE-PEG2000/DSPE-PEG2000- ge11混合胶束。其次，利用纳米快速修复器将CUR-PTX@L与DSPE-PEG2000胶束或DSPE-PEG2000/DSPE-PEG2000- ge11混合胶束进行混合。制备了PEG修饰的姜黄素与紫杉醇脂质体（CUR-PTX@PEG-L）和PEG/ ge11修饰的姜黄素与紫杉醇脂质体（CUR-PTX@GE11-L）。制备荧光脂质体时，分别在脂质乙醇溶液中加入 DID荧光染料。

图：CUR-PTX@GE11-L表征图像

结论：

该文献成功制备出基于DSPE-PEG2000-GE11合成的复合脂质体CUR-PTX@GE11-L。研究表明，复合脂质体CUR-PTX@GE11-L从化合物释放行为、细胞形态变化、肝脏滞留和tumour靶向效率等方面都展现出良好性能。该产品为合理构建智能纳米化合物递送系统提供新的思路。