MRI-visible liposome nanovehicles for potential tumor-targeted delivery of multimodal therapies
MRI-visible liposome nanovehicles for potential tumor-targeted delivery of multimodal therapies
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DOI：
10.1039/c5nr02144h
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发表时间：
2015-01-01
期刊：
影响因子：
6.7
通讯作者：
Zhou, Xin
中科院分区：
文献类型：
--
作者：
Ren, Lili;Chen, Shizhen;Zhou, Xin
通过治疗诊断磁共振成像（MRI），可以实时诊断和监测疾病发展以及对治疗的治疗反应。在这里，我们报告的多功能脂质体的合成，其中包含Gd-DOTA（MRI探针），紫杉醇和c（RGDyk）（靶向肽）。这种纳米颗粒克服了紫杉醇的不溶性，减少了FDA批准的PTX-Cre（Taxol（R））制剂的副作用，并提高了药物向肿瘤的递送效率。c（RGDyk）修饰大大增强了药物在肿瘤细胞A549中的细胞毒性。与非靶向组相比，用靶向脂质体制剂处理的肿瘤细胞中的T-1弛豫率增加了16倍。在体内，施用脂质体后，使用T-I加权成像可视化小鼠中的肿瘤。治疗后肿瘤生长也得到了很好的抑制。体外和离体的荧光图像也显示了这种脂质体在肿瘤细胞中的靶向作用，表明这种纳米载体可以限制抗癌药物和造影剂的脱靶副作用。这些发现为进一步的肿瘤抑制研究和该递送载体在癌症治疗环境中的应用奠定了基础。
Real-time diagnosis and monitoring of disease development, and therapeutic responses to treatment, are possible by theranostic magnetic resonance imaging (MRI). Here we report the synthesis of a multifunctional liposome, which contains Gd-DOTA (an MRI probe), paclitaxel and c(RGDyk) (a targeted peptide). This nanoparticle overcame the insolubility of paclitaxel, reduced the side effects of FDA-approved formulation of PTX-Cre (Taxol (R)) and improved drug delivery efficiency to the tumor.c(RGDyk) modification greatly enhanced the cytotoxicity of the drug in tumor cells A549. The T-1 relaxivity in tumor cells treated with the targeted liposome formulation was increased 16-fold when compared with the non-targeted group. In vivo, the tumors in mice were visualized using T-1-weighted imaging after administration of the liposome. Also the tumor growth could be inhibited well after the treatment. Fluorescence images in vitro and ex vivo also showed the targeting effect of this liposome in tumor cells, indicating that this nanovehicle could limit the off-target side effects of anticancer drugs and contrast agents. These findings lay the foundation for further tumor inhibition study and application of this delivery vehicle in cancer therapy settings.