Characterization, Molecular Docking, and In Vitro Dissolution Studies of Solid Dispersions of 20(S)-Protopanaxadiol
文献类型：期刊论文
| 作者 | Zhang, Qi5,6; Pu, Yiqiong6; Wang, Bing5,6; Wang, Yuqin4; Dong, Tina Tingxia3; Guo, Tao1; Zhang, Tong5,6; Cai, Zhenzhen2 |
| 刊名 | MOLECULES
 |
| 出版日期 | 2017-02 |
| 卷号 | 22期号:2 |
| 关键词 | 20(S)-protopanaxadiol solid dispersion polymer molecular docking in vitro dissolution |
| ISSN号 | 1420-3049 |
| DOI | 10.3390/molecules22020274 |
| 文献子类 | Article |
| 英文摘要 | 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. |
| WOS关键词 | WATER-SOLUBLE DRUG ; IMPROVED ORAL BIOAVAILABILITY ; POLYETHYLENE-GLYCOL 6000 ; ANTIVIRAL AGENT UC-781 ; POLOXAMER 407 ; CANDESARTAN CILEXETIL ; ENHANCED DISSOLUTION ; INTESTINAL BACTERIA ; ANTICANCER ACTIVITY ; GINSENG SAPONIN |
| 资助项目 | National Natural Science Foundation of China[81303233] ; Foundation of Shanghai Science and Technology Commission[13401900300] |
| WOS研究方向 | Biochemistry & Molecular Biology ; Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000395552400088 |
| 出版者 | MDPI AG |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/275645]  |
| 专题 | 药物制剂研究中心 |
| 通讯作者 | Wang, Bing; Cai, Zhenzhen |
| 作者单位 | 1.Chinese Acad Sci, Shanghai Inst Mat Med, Ctr Drug Delivery Syst, Shanghai 201203, Peoples R China; 2.Shanghai Univ Tradit Chinese Med, Expt Ctr Sci & Technol, Shanghai 201203, Peoples R China 3.Hong Kong Univ Sci & Technol, Div Life Sci & Ctr Chinese Med, Hong Kong, Hong Kong, Peoples R China; 4.Zhejiang BioAsia Inst Life Sci, Econ & Tech Dev Zone, 1938 Xinqun Rd, Pinghu 314200, Zhejiang, Peoples R China; 5.Shanghai Univ Tradit Chinese Med, Sch Pharm, Shanghai 201203, Peoples R China; 6.Shanghai Univ Tradit Chinese Med, Expt Ctr Teaching & Learning, Shanghai 201203, Peoples R China; |
| 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.,Dong, Tina Tingxia.,...&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). |
入库方式： OAI收割
来源：上海药物研究所
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