Ze Zhao, Yi Zhao, Chang Chen, Changwei Xie, Ask Verbruggen, E Mccarthy, R Dwyer, L Mcnamara, Z Zhao, Y Zhao, C Xie, C Chen, D Lin, S Wang, B Luo, Y Yuan, Y Zhu, S Liang, R Dong, J Hou, A Isik, A Soran, A Grasi, N Barry, E Sezgin, A Ik, A Grassi, A Soran, Y Yang, Z Zhao, C Xie, Y Zhao, X Zhang, Q Liu, T Zhang, P Gao, H Wang, L Yao, L Hendriks, B Hermans, M Van Den Beuken-Van Everdingen, M Hochstenbag, A Dingemans, Z Zhao, C Chen, C Xie, Y Zhao, X Mu, M Zhang, A Wei, F Yin, Y Wang, K Hu, H Shao, H Shao, P Varamini, S Bose, C Zhang, A Le, Y Zhao, Y Peng, Z Yang, J Lu, R Li, Y Shi, Y Zhao, Z Zhao, Y Cui, X Chen, C Chen, C Xie, F Siyal, Z Memon, R Siddiqui, Z Aslam, U Nisar, R Imad, B Han, Y Yang, J Chen, H Tang, Y Sun, Z Zhang, R Chen, X Chen, Y Zhou, T Lin, Y Leng, X Huang, Y Peng, Y Gao, C Yang, R Guo, X Shi, X Cao, L Zhang, Y Zhao, Q Yue, Q Fu, L Hai, L Guo, M Zhu, X Liu, Y Qu, S Hu, Y Zhang, W Li, J Kim, S Lee, H Kim, Y Choi, J Yoo, K Park
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引用次数: 3
Abstract
Bone metastatic breast cancer is a malignant tumor in bone due to the metastasis of breast cancer, and its incidence is increasing worldwide. Treatment of cancer metastasized to bone is still a challenge because of the anticancer drugs lack target specificity. Finding an effective treatment for bone metastasis remains an urgent issue. In order to enhance the delivery of paclitaxel (PTX) to the bone metastases lesions, a novel glucose derivative was designed and synthesized in this work, which was used as liposome ligand to develop the magnetic liposome G-MLip (Glucose-modified magnetic liposome). The liposome could improve the drug formulations in the bone metastases mediated by glucose transporter 1 (GLUT1) and then target cancer cells. The PTX-loaded magnetic liposome PTX-G-MLip was prepared by the film hydration-ultrasound method. And the characterizations, such as size, zeta potential, encapsulation efficiency, release profile, stability, hemolysis, were well evaluated. What’s more, the enhanced target ability was also investigated in vitro and in mice. The metastatic bone-targeted capacity was confirmed that the PTX concentration from PTX-G-MLip in the bone metastases lesions was markedly increased in the presence of magnetic field (MF) compared with the free PTX and other liposomes. Inspired by the enhanced targeting ability, glucose-modified magnetic liposomes could serve as an effective drug delivery system for targeting and treating bone metastases.
骨转移性乳腺癌是一种因乳腺癌转移而发生在骨内的恶性肿瘤,其发病率在世界范围内呈上升趋势。由于抗癌药物缺乏靶向特异性,骨转移性癌症的治疗仍然是一个挑战。寻找一种有效的骨转移治疗方法仍然是一个迫切的问题。为了增强紫杉醇(PTX)对骨转移病灶的递送,本研究设计并合成了一种新的葡萄糖衍生物,并以其作为脂质体配体制备了磁性脂质体G-MLip (glucose -modified magnetic liposome)。脂质体可以改善葡萄糖转运蛋白1 (GLUT1)介导的骨转移瘤的药物配方,进而靶向癌细胞。采用膜水合超声法制备了PTX-G-MLip磁性脂质体。并对其大小、zeta电位、包封效率、释放谱、稳定性、溶血等特性进行了评价。此外,还在体外和小鼠体内对其增强的靶向能力进行了研究。转移性骨靶向能力证实,与游离PTX和其他脂质体相比,在磁场(MF)存在下,骨转移灶中PTX- g - mlip的PTX浓度明显增加。受其增强的靶向能力的启发,葡萄糖修饰磁性脂质体可以作为一种有效的靶向和治疗骨转移的药物递送系统。
期刊介绍:
EJGO is dedicated to publishing editorial articles in the Distinguished Expert Series and original research papers, case reports, letters to the Editor, book reviews, and newsletters. The Journal was founded in 1980 the second gynaecologic oncology hyperspecialization Journal in the world. Its aim is the diffusion of scientific, clinical and practical progress, and knowledge in female neoplastic diseases in an interdisciplinary approach among gynaecologists, oncologists, radiotherapists, surgeons, chemotherapists, pathologists, epidemiologists, and so on.