Department of Chemical and Biological Engineering, American University of Sharjah, Sharjah, United Arab Emirates.
Materials Science and Engineering Program, American University of Sharjah, Sharjah, United Arab Emirates.
Sci Rep. 2023 Oct 3;13(1):16644. doi: 10.1038/s41598-023-43813-4.
Liposomes are the most successful nanoparticles used to date to load and deliver chemotherapeutic agents to cancer cells. They are nano-sized vesicles made up of phospholipids, and targeting moieties can be added to their surfaces for the active targeting of specific tumors. Furthermore, Ultrasound can be used to trigger the release of the loaded drugs by disturbing their phospholipid bilayer structure. In this study, we have prepared pegylated liposomes using four types of phospholipids with similar saturated hydrocarbon tails including a phospholipid with no head group attached to the phosphate head (DPPA) and three other phospholipids with different head groups attached to their phosphate heads (DPPC, DPPE and DPPG). The prepared liposomes were conjugated to the monoclonal antibody trastuzumab (TRA) to target the human epidermal growth factor receptor 2 (HER2) overexpressed on HER2-positive cancer cells (HER2+). We have compared the response of the different formulations of liposomes when triggered with low-frequency ultrasound (LFUS) and their cellular uptake by the cancer cells. The results showed that the different formulations had similar size, polydispersity, and stability. TRA-conjugated DPPC liposomes showed the highest sensitivity to LFUS. On the other hand, incubating the cancer cells with TRA-conjugated DPPA liposomes triggered with LFUS showed the highest uptake of the loaded calcein by the HER2+ cells.
脂质体是迄今为止最成功的用于将化疗药物装载和递送到癌细胞的纳米颗粒。它们是由磷脂组成的纳米大小的囊泡，可以在其表面添加靶向部分，以对特定肿瘤进行主动靶向。此外，超声可以通过扰乱其磷脂双层结构来触发载药的释放。在这项研究中，我们使用四种具有相似饱和烃尾部的磷脂制备了聚乙二醇化脂质体，包括一种没有头部基团连接到磷酸头部的磷脂（DPPA）和三种具有不同头部基团连接到磷酸头部的其他磷脂（DPPC、DPPE 和 DPPG）。制备的脂质体与曲妥珠单抗（TRA）连接，以靶向在 HER2 阳性癌细胞（HER2+）上过表达的人表皮生长因子受体 2（HER2）。我们比较了不同配方的脂质体在低频超声（LFUS）触发下的反应及其被癌细胞摄取的情况。结果表明，不同配方具有相似的大小、多分散性和稳定性。TRA 缀合的 DPPC 脂质体对 LFUS 最敏感。另一方面，用 LFUS 触发的 TRA 缀合的 DPPA 脂质体孵育癌细胞显示出对负载钙黄绿素的摄取最高。
