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首页> 外文期刊>Molecules >20( S )-Protopanaxadiol Phospholipid Complex: Process Optimization, Characterization, In Vitro Dissolution and Molecular Docking Studies
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20( S )-Protopanaxadiol Phospholipid Complex: Process Optimization, Characterization, In Vitro Dissolution and Molecular Docking Studies

机译：20（S）-原人参二醇二醇复合物：工艺优化，表征，体外溶出和分子对接研究

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20( S )-Protopanaxadiol (PPD), a bioactive compound extracted from ginseng, possesses cardioprotective, neuroprotective, anti-inflammatory, antiestrogenic, anticancer and anxiolytic effects. However, the clinical application of PPD is limited by its weak aqueous solubility. In this study, we optimized an efficient method of preparing its phospholipid complex (PPD-PLC) using a central composite design and response surface analysis. The prepared PPD-PLC was characterized by differential scanning calorimetric, powder X-ray diffraction, Fourier-transformed infrared spectroscopy and nuclear magnetic resonance analyses associated with molecular docking calculation. The equilibrium solubility of PPD-PLC in water and n -octanol increased 6.53- and 1.53-times, respectively. Afterwards, using PPD-PLC as the intermediate, the PPD-PLC-loaded dry suspension (PPD-PLC-SU) was prepared with our previous method. In vitro evaluations were conducted on PPD-PLC and PPD-PLC-SU, including dissolution behaviors and stability properties under different conditions. Results of in vitro dissolution behavior revealed the improved dissolution extents and rates of PPD-PLC and PPD-PLC-SU ( p < 0.05). Results of the formulation stability investigation also exposed the better stability of PPD-PLC-SU compared with free PPD. Therefore, phospholipid complex technology is a useful formulation strategy for BCS II drugs, as it could effectively improve their hydrophilicity and lipophilicity.
机译：从人参中提取的生物活性化合物20（S）-普萘他那二醇（PPD）具有心脏保护，神经保护，抗炎，抗雌激素，抗癌和抗焦虑的作用。但是，PPD的临床应用受到其弱的水溶性的限制。在这项研究中，我们优化了使用中央复合材料设计和响应面分析制备其磷脂复合物（PPD-PLC）的有效方法。通过差示扫描量热，粉末X射线衍射，傅立叶变换红外光谱和与分子对接计算相关的核磁共振分析对所制备的PPD-PLC进行表征。 PPD-PLC在水和正辛醇中的平衡溶解度分别增加了6.53和1.53倍。然后，使用PPD-PLC作为中间体，用我们以前的方法制备了装载PPD-PLC的干悬浮液（PPD-PLC-SU）。在PPD-PLC和PPD-PLC-SU上进行了体外评估，包括在不同条件下的溶解行为和稳定性。体外溶出行为的结果表明，PPD-PLC和PPD-PLC-SU的溶出程度和溶出率均有改善（p <0.05）。制剂稳定性研究的结果还显示，与游离PPD相比，PPD-PLC-SU具有更好的稳定性。因此，磷脂络合物技术是BCS II药物的有用的配制策略，因为它可以有效地改善其亲水性和亲脂性。

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