Studies on tissue distribution of scutellarin and methyl polyethylene glycol (mPEG)-scutellarin prodrug in mice

详细信息	查看全文 | 推荐本文 |

• 作者：Juan Lu<sup>asup> ; Xia Zhan<sup>bsup> ; Qingfei Liu<sup>csup> ; Xi Chen<sup>asup><sup> ; sup><sup>chenxi@implad.ac.cnsup> ; Xinge Zhao<sup>dsup> ; Yiming Wang<sup>csup> ; Guoan Luo<sup>csup><sup> ; sup><sup>luoga@mail.tsinghua.edu.cnsup>
• 关键词：PEGylation ; Scutellarin ; Tissue distribution ; Cerebral I/R injury ; Brain-targeting
• 刊名：Acta Pharmaceutica Sinica B
• 出版年：2012
• 期刊代码：pca379_22113835
• 类别：pha
• 出版时间：June, 2012
• 卷：2
• 期：3
• 页码：274-277
• 文件大小：378 K

摘要

This study was to determine tissue distribution and pharmacokinetics of mPEG-scutellarin prodrug (<strong class="boldFont">7estrong>), a chemical entity previously shown to have a beneficial effect in cerebral ischemia/reperfusion (I/R) injury. After injecting scutellarin or prodrug <strong class="boldFont">7estrong>, the concentrations of scutellarin and <strong class="boldFont">7estrong> in tissues were determined and the pharmacokinetic parameters were calculated. The results showed that the distribution of scutellarin in tissues was enhanced by PEGylation. The distribution of <strong class="boldFont">7estrong> in brain was approximately 2.1-fold higher than that of scutellarin, indicating that PEGylation increased the brain penetration of scutellarin. We conclude that <strong class="boldFont">7estrong> could exert more effective protection on cerebral I/R injury in mice. This study also provided a simple and convenient strategy to identify novel drugs with potential protective function for I/R injury in mice.