• 主题
高级搜索  >
历史搜索 清空历史
首页> 外文期刊>RSC Advances >Improved oral bioavailability of docetaxel by nanostructured lipid carriers: in vitro characteristics, in vivo evaluation and intestinal transport studies
【24h】

Improved oral bioavailability of docetaxel by nanostructured lipid carriers: in vitro characteristics, in vivo evaluation and intestinal transport studies

机译：通过纳米结构脂质载体改善多西紫杉醇的口服生物利用度：体外特征，体内评估和肠道运输研究

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

The objective of the current study was to explore the potential of nanostructured lipid carriers (NLC) for oral delivery of docetaxel (DTX) and investigate the absorption mechanism in vivo. Docetaxel-loaded nanostructured lipid carriers (DNLCs) were prepared by emulsification-ultrasonication and their physicochemical properties were characterized. Differential scanning calorimetry (DSC) demonstrated that the drug was present in a amorphous state and FTIR analysis suggested that the interaction of DTX and lipids involved hydrogen bonding and hydrophobic interactions. DNLCs were found to be stable in simulated gastrointestinal fluids and in vitro drug release studies revealed that the formulation exhibited sustained drug release for 48 h by Fickian diffusion. The drug absorption in the intestine was markedly improved by NLCs. An in vivo pharmacokinetic study demonstrated that the AUC(0-24) (h) for DNLCs (536.18 +/- 91.21 ng mL(-1) h) was increased 4.31-fold compared with that of docetaxel solution (DTX-Sol). DNLCs could be absorbed into the enterocytes through both endocytosis and passive transport. The oral bioavailability of DNLCs was significantly reduced after the lymphatic transport pathway was blocked. The overall results showed that the NLCs were a very effective method for increasing the oral absorption of docetaxel.
机译：目前研究的目的是探讨用于口服多西紫杉醇（DTX）的纳米结构脂质载体（NLC）的潜力，并研究体内的吸收机制。通过乳化 - 超声处理制备多西紫杉醇负载纳米结构脂质载体（DNLC），其物理化学性质表征。差分扫描量热法（DSC）证明该药物以无定形状态存在，FTIR分析表明DTX和脂质的相互作用涉及氢键和疏水相互作用。发现DNLC在模拟的胃肠液中稳定，体外药物释放研究表明，制剂通过Fickian扩散表现出48小时的持续药物释放。 NLCs的肠道中的吸毒性显着改善。体内药代动力学研究证明，与多西紫杉醇溶液（DTX-溶胶）相比，DNLCS（536.18 +/- 91.21 ng ml（-1）h）的AUC（0-24）（H）增加了4.31倍。 DNLC可以通过内吞作用和被动运输吸收到肠细胞中。在淋巴输送途径阻断后，DNLC的口腔生物利用度显着降低。总体结果表明，NLC是增加多西紫杉醇口服吸收的非常有效的方法。

著录项

  • 来源
    《RSC Advances》 |2015年第117期|共11页
  • 作者

    Fang Guihua; Tang Bo; Chao Yanhui; Zhang Yu; Xu Hui; Tang Xing;

  • 作者单位

    Shenyang Pharmaceut Univ Sch Pharm Shenyang 110016 Peoples R China;

    Shenyang Pharmaceut Univ Sch Pharm Shenyang 110016 Peoples R China;

    Shenyang Pharmaceut Univ Sch Pharm Shenyang 110016 Peoples R China;

    Shenyang Pharmaceut Univ Sch Pharm Shenyang 110016 Peoples R China;

    Shenyang Pharmaceut Univ Sch Pharm Shenyang 110016 Peoples R China;

    Shenyang Pharmaceut Univ Sch Pharm Shenyang 110016 Peoples R China;

  • 收录信息
  • 原文格式 PDF
  • 正文语种 eng
  • 中图分类 化学;
  • 关键词

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