Department of Oncology, Shanghai Pudong New Area People's Hospital, Shanghai, 201200, China.
Department of Oncology, Changhai Hospital Affiliated To Navy Medical University, Shanghai, 200433, China.
Sci Rep. 2022 Feb 16;12(1):2610. doi: 10.1038/s41598-022-06677-8.
Due to the presence of the blood-brain barrier (BBB), the delivery of general drugs into the brain tissue remains to be a tricky problem. For patients with brain metastases from breast cancer, drug delivery systems must overcome this physical barrier. Targeted nano vehicles arise as a promising alternative to deliver drugs to brain tissues successively. Herein, a dual targeting micelle drug delivery system loaded with paclitaxel (PTX) and lapatinib (LPTN) was developed for combinational therapy of brain metastases. In our study, it was shown the micelles modified with Angiopep-2 had high loading efficiency of paclitaxel and lapatinib (Ang-MIC-PTX/LP). In addition, Ang-MIC-PTX/LP could transport across the in vitro BBB model and accumulate in breast cancer cells. After intravenous injection, Ang-MIC significantly accumulated in the brain metastasis. Ang-MIC-PTX/LP could also extend the life span of brain metastasis mouse models. Overall, this study provided a promising method for treatment of brain metastases from breast cancer.
由于血脑屏障（BBB）的存在，将一般药物递送到脑组织仍然是一个棘手的问题。对于患有乳腺癌脑转移的患者，药物递送系统必须克服这一物理屏障。靶向纳米载体作为一种有前途的替代方法，成功地将药物递送到脑组织。在此，我们开发了一种载紫杉醇（PTX）和拉帕替尼（LPTN）的双重靶向胶束药物递送系统，用于脑转移的联合治疗。在我们的研究中，表明用 Angiopep-2 修饰的胶束具有高的紫杉醇和拉帕替尼的载药效率（Ang-MIC-PTX/LP）。此外，Ang-MIC-PTX/LP 可以穿过体外 BBB 模型并在乳腺癌细胞中积累。静脉注射后，Ang-MIC 显著在脑转移部位蓄积。Ang-MIC-PTX/LP 还可以延长脑转移小鼠模型的寿命。总的来说，这项研究为治疗乳腺癌脑转移提供了一种有前途的方法。
