• 主题
高级搜索  >
历史搜索 清空历史
首页> 外文期刊>International Journal of Pharmaceutics >Design of a zero-order sustained release PLGA microspheres for palonosetron hydrochloride with high encapsulation efficiency
【24h】

Design of a zero-order sustained release PLGA microspheres for palonosetron hydrochloride with high encapsulation efficiency

机译：具有高封装效率的盐酸盐蛋白零级持续释放PLGA微球的设计

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

Efficient encapsulation of hydrophilic drugs was substantially challenging when using emulsion solvent evaporation approach. The aim of present study was to design palonosetron hydrochloride-loaded PLGA microspheres (Pal-MS) with high encapsulation efficiency (EE) to sustain drug release for over several days. Pal-MS were prepared using emulsion-solvent evaporation method. Results showed that the pH of external phase could significantly affect the EE and the drug release rate of Pal-MS. By increasing the pH of external phase from 5.0 to 10.0, EE of Pal-MS increased from 55.64% to 94.33%. When the pH of external phase was 7.0, an ideal Pal-MS with EE of 86.51% and a zero-order drug release profile was obtained. The improved EE and drug release performance was proved to be associated with possible PLGA degradation, enhanced drug-PLGA interaction and reduced drug diffusion from organic phase to aqueous phase. After subcutaneous injection, such Pal-MS showed more steady drug plasma concentration (0.207-1.238 ng/ml) over the entire 6-day in comparison with those of multiple-day-dosing intravenous palonosetron hydrochloride solution. It was concluded that Pal-MS were successfully designed by the adjustment of the pH of external phase and could be promising for preventing both acute and delayed chemotherapy-induced nausea and vomiting (CINV).
机译：当使用乳液溶剂蒸发方法时，亲水性药物的有效封装显着挑战。目前研究的目的是以高封装效率（EE）设计Palonosetron负载的PLGA微球（PAL-MS）以维持药物释放超过几天。使用乳液 - 溶剂蒸发方法制备PAL-MS。结果表明，外部阶段的pH可以显着影响ee和PAL-MS的药物释放速率。通过从5.0至10.0增加外部阶段的pH值，PAL-MS的EE从55.64％增加到94.33％。当外阶段的pH为7.0时，获得了EE的理想PAL-MS为86.51％和零级药物释放曲线。证明了改善的EE和药物释放性能与可能的PLGA降解，增强的药物 - PLGA相互作用和从有机相中减少到水相中的药物扩散。在皮下注射后，与多日给药静脉静脉静脉酮溶液相比，这种PAL-MS在整个6天内显示出更稳定的药物血浆浓度（0.207-1.238ng / ml）。得出结论，PAL-MS通过调整外部阶段的pH成功设计，并且可以预防急性和延迟化疗诱导的恶心和呕吐（CINV）。

著录项

  • 来源
    《International Journal of Pharmaceutics》 |2020年第2020期|共12页
  • 作者

    Yang Ziyi; Liu Lu; Su Lili; Wu Xueqing; Wang Yicheng; Liu Lei; Lin Xia;

  • 作者单位

    Jiangnan Univ Sch Pharmaceut Sci 1800 Lihu Rd Wuxi 214122 Jiangsu Peoples R China;

    Jiangnan Univ Sch Pharmaceut Sci 1800 Lihu Rd Wuxi 214122 Jiangsu Peoples R China;

    Jiangnan Univ Sch Pharmaceut Sci 1800 Lihu Rd Wuxi 214122 Jiangsu Peoples R China;

    Jiangnan Univ Sch Pharmaceut Sci 1800 Lihu Rd Wuxi 214122 Jiangsu Peoples R China;

    Jiangnan Univ Sch Pharmaceut Sci 1800 Lihu Rd Wuxi 214122 Jiangsu Peoples R China;

    Jiangnan Univ Sch Pharmaceut Sci 1800 Lihu Rd Wuxi 214122 Jiangsu Peoples R China;

    Jiangnan Univ Sch Pharmaceut Sci 1800 Lihu Rd Wuxi 214122 Jiangsu Peoples R China;

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

    Palonosetron hydrochloride; PLGA microspheres; Sustained release; CINV;

    机译：Palonosetron盐酸盐;PLGA微球;持续释放;CINV;

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