Phytosome-nanosuspensions for silybin-phospholipid complex with increased bioavailability and hepatoprotection efficacy.,European Journal of Pharmaceutical Sciences

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Phytosome-nanosuspensions for silybin-phospholipid complex with increased bioavailability and hepatoprotection efficacy.
European Journal of Pharmaceutical Sciences ( IF 4.3 ) Pub Date : 2020-01-08 , DOI: 10.1016/j.ejps.2020.105212
Cheng Chi ₁ , Chenshuang Zhang ₁ , Yang Liu ₁ , Haichen Nie ₂ , Jianping Zhou ₁ , Yang Ding ₁

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Silybin, a natural compound for treating liver disease, has been shown to provide diverse biological activities such as anticancer, antioxidant and hepatoprotective. However, it is still challenging to develop silybin product due to its poor aqueous solubility and limited gastrointestinal absorption. In order to improve the low bioavailability of silybin, a novel formulation of phytosome-nanosuspensions for silybin shielding termed as SPCs-NPs, has been developed herein for hepatoprotection efficacy. We found that SPCs-NPs formulation not only possessed an increased in vitro dissolution rate but also improved plasma concentration in the in vivo pharmacokinetic study. Moreover, SPCs-NPs was provided with more potent hepatoprotective effects in pharmacodynamic assessments. Moreover, physicochemical features including interactions between silybin and phospholipid, and crystalline variation of the optimized SPCs-NPs formulation were confirmed by using Fourier-transform infrared spectrometry (FTIR), 1H nuclear magnetic resonance spectroscopy (H-NMR), differential scanning calorimetry (DSC), and powder X-ray diffraction spectroscopy (PXRD) respectively. Overall, the interesting finding of this study suggested that SPCs-NPs could be applied as a promising formulation for a higher drug bioavailability and better hepatoprotection efficacy.

中文翻译：

水飞蓟宾-磷脂复合物的植物脂质体悬浮液，具有更高的生物利用度和保肝功效。

水飞蓟宾是治疗肝脏疾病的天然化合物，已显示出提供多种生物活性，例如抗癌，抗氧化剂和保肝作用。然而，由于水飞蓟宾的水溶性差且胃肠道吸收有限，因此开发水飞蓟宾产品仍然具有挑战性。为了改善水飞蓟宾的低生物利用度，本文已经开发了用于水飞蓟宾保护的植物体-纳米悬浮液的新制剂，其被称为SPCs-NP，具有保肝作用。我们发现，在体内药代动力学研究中，SPCs-NPs制剂不仅具有更高的体外溶出速率，而且具有更高的血浆浓度。此外，在药效学评估中，SPCs-NPs具有更强的肝保护作用。此外，通过傅立叶变换红外光谱（FTIR），1H核磁共振波谱（H-NMR），差示扫描量热法（DSC），和粉末X射线衍射光谱法（PXRD）。总的来说，这项研究的有趣发现表明，SPCs-NPs可以作为有前途的制剂用于更高的药物生物利用度和更好的保肝功效。和粉末X射线衍射光谱法（PXRD）。总的来说，这项研究的有趣发现表明，SPCs-NPs可以作为有前途的制剂用于更高的药物生物利用度和更好的保肝功效。和粉末X射线衍射光谱法（PXRD）。总的来说，这项研究的有趣发现表明，SPCs-NPs可以作为有前途的制剂用于更高的药物生物利用度和更好的保肝功效。

更新日期：2020-01-08

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