Magnolol, which is a CYP3A substrate, is a well-known agent that can facilitate neuroprotection and reduce ischemic brain damage. However, a well-controlled release formulation is needed for the effective delivery of magnolol due to its poor water solubility. In this study, we have developed a formulation for a CYP3A-excipient microemulsion, which can be administrated intraperitoneally to increase the solubility and bioavailability of magnolol and increase its neuroprotective effect against ischemic brain injury. The results showed a significant improvement in the area under the plotted curve of drug concentration versus time curve (AUC0–t) and mean residence time (MRT) of magnolol in microemulsion compared to when it was dissolved in dimethyl sulfoxide (DMSO). Both magnolol in DMSO and microemulsion, administrated after the onset of ischemia, showed a reduced visual brain infarct size. As such, this demonstrates a therapeutic effect on ischemic brain injury caused by occlusion, however it is important to note that a pharmacological effect cannot be concluded by this study. Ultimately, our study suggests that the excipient inhibitor-based microemulsion formulation could be a promising concept for the substrate drugs of CYP3A.

中文翻译：

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CYP3A赋形剂基微乳剂延长了Magnolol对缺血性中风大鼠的作用。

Magnolol是一种CYP3A底物，是众所周知的药物，可以促进神经保护作用并减少缺血性脑损伤。然而，由于厚朴酚的水溶性差，因此需要有效控制释放的制剂来有效递送厚朴酚。在这项研究中，我们开发了一种用于CYP3A赋形剂的微乳剂，可以腹膜内给药以增加厚朴酚的溶解度和生物利用度，并提高其对缺血性脑损伤的神经保护作用。结果显示，与溶解在二甲亚砜（DMSO）中相比，厚朴酚在微乳液中的药物浓度与时间曲线（AUC0–t）和平均停留时间（MRT）的绘制曲线下的面积有了显着改善。DMSO和微乳中的厚朴酚均在缺血发作后给药，显示出减少的视觉脑梗死面积。因此，这证明了对由闭塞引起的缺血性脑损伤的治疗作用，但是重要的是要注意，该研究不能得出药理作用的结论。最终，我们的研究表明，基于赋形剂抑制剂的微乳制剂可能是CYP3A底物药物的一个有前途的概念。