...
  • 主题
高级搜索  >
历史搜索 清空历史
首页> 外文期刊>Drug Design, Development and Therapy >A novel glycyrrhetinic acid-modified oxaliplatin liposome for liver-targeting and in vitro/vivo evaluation
【24h】

A novel glycyrrhetinic acid-modified oxaliplatin liposome for liver-targeting and in vitro/vivo evaluation

机译：新型甘草次酸修饰的奥沙利铂脂质体用于肝靶向和体外/体内评价

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

摘要

Abstract: In this study, oxaliplatin (OX) liposomes surface-modified with glycyrrhetinic acid (GA) were developed by the film-dispersion method. Their morphology, physical and chemical properties, and in vitro release performance were investigated. The transmission electron microscope (TEM) image showed that most liposomes were spherical particles with similar size and uniform dispersion. Both OX-liposomes and GA-OX-liposomes had an average size of 90 nm. They were negatively charged, with zeta potentials of -20.6 and -21.3 mV, respectively, and the entrapment efficiency values of both were higher than 94%. In vitro data showed that the application of liposomes could prolong the OX release. The relatively high correlation coefficient values obtained from analyzing the amount of drug released versus the square root of time depicted that release followed the Weibull model. No significant changes were observed after the addition of GA to the liposomes. In vivo, the relatively long time to reach the maximum plasma concentration of OX-liposomes suggested a sustained-release profile of liposomes, which was consistent with the results of the in vitro release study. The increased area under the curve and maximum plasma concentration of OX-liposomes and GA-OX-liposomes demonstrated an increased absorption. The drug concentration in tissues indicated that the GA-modified liposomes delivered OX mainly to liver after intravenous administration. In addition, no severe signs, such as appearance of epithelial necrosis or sloughing of epithelial cells, were detected in histology studies.
机译：摘要：本研究通过膜分散法开发了用甘草次酸（GA）表面改性的奥沙利铂（OX）脂质体。研究了它们的形态，理化性质和体外释放性能。透射电子显微镜（TEM）图像显示，大多数脂质体为球形颗粒，大小相似且分散均匀。 OX-脂质体和GA-OX-脂质体均具有90nm的平均尺寸。它们带负电，ζ电位分别为-20.6和-21.3 mV，两者的包封效率均高于94％。体外数据表明，脂质体的应用可以延长OX的释放。通过分析药物释放量相对于时间的平方根获得的相对较高的相关系数值描述了遵循Weibull模型的药物释放。将GA加入脂质体后，未观察到明显变化。在体内，达到OX-脂质体最大血浆浓度的时间相对较长，这表明脂质体具有持续释放的特性，这与体外释放研究的结果一致。曲线下的增加的面积和OX-脂质体和GA-OX-脂质体的最大血浆浓度显示出增加的吸收。组织中的药物浓度表明，GA修饰的脂质体在静脉内给药后主要将OX递送至肝脏。另外，在组织学研究中未检测到严重的迹象，例如上皮坏死的出现或上皮细胞的脱落。

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