Lin Wen, Xie Xiangyang, Yang Yanfang, Fu Xudong, Liu Hong, Yang Yang, Deng Jianping
a Department of Clinical Laboratory , Huangshi Love & Health Hospital of Hubei Province , Huangshi , P.R. China.
b Department of Pharmacy , Wuhan General Hospital of Guangzhou Military Command , Wuhan , P.R. China.
Drug Deliv. 2016 Nov;23(9):3436-3443. doi: 10.1080/10717544.2016.1189983. Epub 2016 Jun 7.
To specifically deliver cytotoxic drug to tumor cells and enhance cellular uptake is the key for effective cancer therapy. In this paper, we described a novel drug targeting system, which is designed to combine features of biological (cell-penetrating peptides, CPPs) and physical (magnetic) drug targeting for use in the magnetic hyperthermia-triggered release. A doxorubicin-CPPs conjugate (DOX-CPPs) was loaded into thermosensitive magnetic liposomes (TSMLs) (DOX-CPPs/TSMLs), and in vitro DOX-CPPs thermosensitive release activity, anti-proliferation effect, in vivo targeted delivery as well as in vivo antitumor activity were determined. The results demonstrated that the DOX-CPPs/TSMLs showed good physicochemical properties, effective anti-proliferation effect in MCF-7 cells in vitro. Additionally, in vivo study, DOX-CPPs/TSMLs under AC magnetic field displayed superior in vivo targeted delivery efficacy, antitumor efficacy in an MCF-7 xenograft murine model. In conclusion, the application of DOX-CPPs/TSMLs under AC magnetic field may provide a strategy for the selective and efficient delivery of drug.
将细胞毒性药物特异性递送至肿瘤细胞并增强细胞摄取是有效癌症治疗的关键。在本文中，我们描述了一种新型药物靶向系统，该系统旨在结合生物（细胞穿透肽，CPPs）和物理（磁性）药物靶向的特性，用于磁热疗触发释放。将阿霉素-CPPs缀合物（DOX-CPPs）负载到热敏磁性脂质体（TSMLs）中（DOX-CPPs/TSMLs），并测定了体外DOX-CPPs热敏释放活性、抗增殖作用、体内靶向递送以及体内抗肿瘤活性。结果表明，DOX-CPPs/TSMLs具有良好的理化性质，在体外对MCF-7细胞具有有效的抗增殖作用。此外，在体内研究中，DOX-CPPs/TSMLs在交变磁场下在MCF-7异种移植小鼠模型中显示出优异的体内靶向递送效果和抗肿瘤效果。总之，在交变磁场下应用DOX-CPPs/TSMLs可能为药物的选择性和高效递送提供一种策略。
