...
  • 主题
高级搜索  >
历史搜索 清空历史
首页> 外文期刊>Biomedicine & pharmacotherapy =: Biomedecine & pharmacotherapie >Paclitaxel-loaded folate-coated long circulating and pH-sensitive liposomes as a potential drug delivery system: A biodistribution study
【24h】

Paclitaxel-loaded folate-coated long circulating and pH-sensitive liposomes as a potential drug delivery system: A biodistribution study

机译：紫杉醇加载的叶酸叶酸长循环和pH敏感的脂质体作为潜在的药物递送系统：生物分布研究

获取原文
获取原文并翻译 | 示例
   

获取外文期刊封面封底 >>

       
页面导航
  • 摘要
  • 著录项
  • 相似文献
  • 相关主题

摘要

A range of antitumor agents for cancer treatment is available; however, they show low specificity, which often limit their use. Recently, we have reported the preparation of folate-coated long-circulating and pH-sensitive liposomes (SpHL-folate-PTX) loaded with paclitaxel (PTX), an effective drug for the treatment of solid tumors, including breast cancer. The purpose of this study was to prepare and characterize SpHL-PTX and SpHL-folate-PTX radiolabeled with technetium-99 m (Tc-99m). Biodistribution studies and scintigraphic images were performed after intravenous administration of Tc-99m-PTX, Tc-99m-SpHL-PTX and Tc-99m-SpHL-folate-PTX into healthy and tumor-bearing mice. High radiochemical purity (98%) and in vitro stability (90%) were achieved for both liposome formulations. The pharmacokinetic properties of Tc-99m-SpHL-DTPA-PTX and Tc-99m-SpHL-folate-DTPA-PTX decreased in a monophasic manner showing half-life of 400.1 and 541.8 min, respectively. Scintigraphic images and biodistribution studies showed a significant uptake in liver, spleen and kidneys, demonstrating these routes as way for excretion. At 8 h post-injection, the liposomal tumor uptake was higher than Tc-99m-PTX. Interesting, 4 h after administration, the liposome folate coated showed higher tumor-to-muscle ratio than Tc-99m-SpHL-DTPA-PTX and Tc-99m-PTX. In conclusion, the liposomal systems, showed high tumor uptake by scintigraphic images, especially the Tc-99m-SpHL-folate-DTPA-PTX that showed a sustained and higher tumor-to-muscle ratio than non-functionalized liposome, which indicate its feasibility as a PTX delivery system to folate positive tumors.
机译：可获得一系列癌症治疗的抗肿瘤剂;然而，它们表现出低特异性，这通常限制了他们的使用。最近，我们已经报道了制备叶酸涂层的长循环和pH敏感的脂质体（SPHL-叶酸-PTX），其装有紫杉醇（PTX），是治疗固体瘤的有效药物，包括乳腺癌。本研究的目的是准备和表征与TechNetium-99M（TC-99M）放射性标记的SPHL-PTX和SPHL-叶酸-PTX。在静脉内施用TC-99M-PTX，TC-99M-PTX，TC-99M-SPHL-叶酸-PTX进入健康和肿瘤的小鼠之后进行生物分布研究和闪烁图像。对于脂质体配方，实现了高放射化学纯度（＆ 98％）和体外稳定性（＆ 90％）。 TC-99M-SPHL-DTPA-PTX和TC-99M-SPHL-叶酸DTPA-PTX的药代动力学性质以单极的方式降低，显示出400.1和541.8分钟的半衰期。闪烁的图像和生物分布研究表明肝脏，脾和肾脏的显着摄取，以排泄方式展示这些途径。在注射后8小时，脂质体肿瘤摄取高于TC-99m-PTX。施用4小时，脂质体叶酸涂层显示出比TC-99M-SPHL-DTPA-PTX和TC-99M-PTX较高的肿瘤肌肉比。总之，脂质体系统显示闪烁图像的高肿瘤摄取，尤其是表现出持续和更高的肿瘤至肌肉比的TC-99M-SPHL-叶酸-DTPA-PTX表明其可行性作为叶酸阳性肿瘤的PTX递送系统。

著录项

相似文献

  • 外文文献
  • 中文文献
  • 专利
获取原文

客服邮箱：kefu@zhangqiaokeyan.com

京公网安备：11010802029741号 ICP备案号：京ICP备15016152号-6 六维联合信息科技 (北京) 有限公司©版权所有

  • 客服微信

  • 服务号