• 主题
高级搜索  >
历史搜索 清空历史
首页> 外文期刊>Journal of Applied Polymer Science >Improved stability and tumor targeting of 5-fluorouracil by conjugation with hyaluronan
【24h】

Improved stability and tumor targeting of 5-fluorouracil by conjugation with hyaluronan

机译：与透明质酸结合提高了5-氟尿嘧啶的稳定性和靶向性

获取原文
获取原文并翻译 | 示例
           
页面导航
  • 摘要
  • 著录项
  • 相似文献
  • 相关主题

摘要

To circumvent the rapid clearance in vivo and consequent low tumor targeting of 5-fluorouracil (5-Fu), hyaluronan-5-fluorouracil conjugate (HA-5-Fu) was firstly synthesized and characterized. The stability of HA-5-Fu in vitro was evaluated by incubation with phosphate buffered saline, hyaluronidase solution, and mice plasma, respectively. The tumor targeting was tested by in vitro cytotoxicity evaluation and in vivo pharmacokinetics study in plasma and tumor. HA-5-Fu with drug loading of 87.674 mg/g was successfully obtained and confirmed. HA-5-Fu showed high stability in acidic environment and moderate stability under enzymatic cleavage. The enhanced cytotoxicity of HA-5-Fu over 5-Fu depended on drug concentration, incubation time, and cell lines type. The t_(1/2) of HA-5-Fu in plasma after injection of prodrug was extended up to 10 times compared with that of 5-Fu. Notably, AUC0-t in tumors of HA-5-Fu was 3.6 times higher than 5-Fu, demonstrating its excellent tumor targeting and quite promising prospect in anti-cancer therapy.
机译：为了规避体内5-氟尿嘧啶（5-Fu）的快速清除和随之而来的低肿瘤靶向性，首先合成并表征了透明质酸-5-氟尿嘧啶缀合物（HA-5-Fu）。通过分别与磷酸盐缓冲液，透明质酸酶溶液和小鼠血浆一起孵育来评估HA-5-Fu的体外稳定性。通过体外细胞毒性评估以及在血浆和肿瘤中的体内药代动力学研究来测试肿瘤靶向。成功获得并确认了载药量为87.674 mg / g的HA-5-Fu。 HA-5-Fu在酸性环境中显示出很高的稳定性，而在酶促裂解下表现出中等的稳定性。 HA-5-Fu相对于5-Fu增强的细胞毒性取决于药物浓度，孵育时间和细胞系类型。注射前药后血浆中HA-5-Fu的t_（1/2）扩展到10倍，是5-Fu。值得注意的是，HA-5-Fu肿瘤中的AUC0-t是5-Fu的3.6倍，这表明其出色的靶向性和抗癌治疗的前景十分可观。

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