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Characterization, Molecular Docking, and In Vitro Dissolution Studies of Solid Dispersions of 20(S)-Protopanaxadiol 期刊论文

编号：

f8000a8c-6bd0-4499-a566-2f182d79fbfe
作者：

Zhang, Qi(张琦)#^[1,2]Pu, Yiqiong(浦益琼)#^[1]Wang, Bing(王冰)*^[1,2]Wang, Yuqin^[3];Dong, Tina Tingxia^[4];Guo, Tao^[5];Zhang, Tong(张彤)^[1,2]Cai, Zhenzhen(蔡贞贞)*^[6]
语种：

英文
期刊：

MOLECULES ISSN：1420-3049 2017 年 22 卷 2 期 ; FEB
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关键词：

20(S)-protopanaxadiol solid dispersion polymer molecular docking in vitro dissolution
摘要：

In this study, we prepared solid dispersions (SDs) of 20(S)-protopanaxadiol (PPD) using a melting-solvent method with different polymers, in order to improve the solubility and dissolution performance of drugs with poor water solubility. The SDs were characterized via differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD), Fourier transform infrared spectroscopy (FTIR), nuclear magnetic resonance (NMR), and molecular docking and dynamics study. DSC and PXRD results indicated that PPD crystallinity in SDs was significantly reduced, and that the majority of PPD is amorphous. No interaction was observed between PPD and polymers on FTIR and NMR spectra. Molecular docking and dynamic calculations indicated that the PPD molecule localized to the interpolated charged surface, rather than within the amorphous polymer chain network, which might help prevent PPD crystallization, consequently enhancing the PPD dispersion in polymers. An in vitro dissolution study revealed that the SDs considerably improved the PPD dissolution performance in distilled water containing 0.35% Tween-80 (T-80). Furthermore, among three PPD-SDs formulations, Poloxamer188 (F68) was the most effective in improving the PPD solubility and was even superior to the mixed polymers. Therefore, the SD prepared with F68 as a hydrophilic polymer carrier might be a promising strategy for improving solubility and in vitro dissolution performance. F68-based SD, containing PPD with a melting-solvent preparation method, can be used as a promising, nontoxic, quick-release, and effective intermediate for other pharmaceutical formulations, in order to achieve a more effective drug delivery.
推荐引用方式
GB/T 7714：

Zhang Qi,Pu Yiqiong,Wang Bing, et al. Characterization, Molecular Docking, and In Vitro Dissolution Studies of Solid Dispersions of 20(S)-Protopanaxadiol [J].MOLECULES,2017,22(2).
APA：

Zhang Qi,Pu Yiqiong,Wang Bing,Wang Yuqin,&Cai Zhenzhen.(2017).Characterization, Molecular Docking, and In Vitro Dissolution Studies of Solid Dispersions of 20(S)-Protopanaxadiol .MOLECULES,22(2).
MLA：

Zhang Qi, et al. "Characterization, Molecular Docking, and In Vitro Dissolution Studies of Solid Dispersions of 20(S)-Protopanaxadiol" .MOLECULES 22,2(2017).
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