Modified Release and Improved Stability of Unstable BCS II Drug by Using Cyclodextrin Complex as Carrier To Remotely Load Drug into Niosomes
文献类型：期刊论文
| 作者 | Chi, Liandi1; Wu, Delin2; Li, Zhuo1,3; Zhang, Minmin4 ; Liu, Hongchun4; Wang, Caifen1; Gui, Shuangying2; Geng, Meiyu4; Li, Haiyan1; Zhang, Jiwen1,2
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| 刊名 | MOLECULAR PHARMACEUTICS
 |
| 出版日期 | 2016-01 |
| 卷号 | 13期号:1页码:113-124 |
| 关键词 | niosomes pseudolaric acid B remote loading pH gradient retarded release enzymatic stability |
| ISSN号 | 1543-8384 |
| DOI | 10.1021/acs.molpharmaceut.5b00566 |
| 文献子类 | Article |
| 英文摘要 | In answering to the challenge of enzymatic unstability of Biopharmaceutics Classification System (BCS) class II drugs, an effective remote loading strategy was developed to successfully incorporate the drug cyclodextrin (CD) complex into niosomes to modify the release and stability of a drug candidate, pseudolaric acid B (PAB). Judged by binding constants, and combined solubilization effects of pH and CD complexation on PAB at different pH, the complex internalization driven by a transmembrane pH gradient (from 2.0 to 7.4) and the dynamic shifting of PAB CD complexation equilibrium at this gradient were introduced. The transfer of PAB CD complex into the internal aqueous phase of niosomes at 60 degrees C was primarily verified by synchrotron radiation Fourier transform infrared spectroscopy. The remote loading samples behaved as retarded release at pH 5.8, 6.8, and 7.4, for which the stability of PAB in rat plasma was significantly enhanced (about 8.1-fold), in comparison with niosomes prepared by the passive and lipid bilayer loading of PAB. The drug carrier interaction based release modeling was further fitted, and the convection rate constant (k(s)) and free energy difference between free and bound states (Delta G) indicated the strongest PAB carrier interactions in remote loading niosomes. The remote loading strategy also reduced the CD cholesterol interaction and provided better physical stability of the system. In conclusion, the remote loading of drug CD complex into niosomes provides advantages to modify the release and enhance the stability of unstable BCS class II drug. |
| WOS关键词 | PSEUDOLARIC-ACID-B ; HYDROXYPROPYL-BETA-CYCLODEXTRIN ; INCLUSION COMPLEXES ; IN-VITRO ; TOPICAL DELIVERY ; INHIBITS ANGIOGENESIS ; INSOLUBLE DRUGS ; LIPID RAFTS ; LIPOSOMES ; VIVO |
| 资助项目 | Natural Science Foundation of China[81430087] ; Natural Science Foundation of China[81373358] |
| WOS研究方向 | Research & Experimental Medicine ; Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000367866200012 |
| 出版者 | AMER CHEMICAL SOC |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/276266]  |
| 专题 | 药理学第一研究室 中科院受体结构与功能重点实验室 新药研究国家重点实验室 药物制剂研究中心 |
| 通讯作者 | Zhang, Jiwen |
| 作者单位 | 1.Chinese Acad Sci, Shanghai Inst Mat Med, Ctr Drug Delivery Syst, Shanghai 201210, Peoples R China; 2.Anhui Univ Chinese Med, Sch Pharmaceut Sci, Hefei 230038, Peoples R China; 3.Shenyang Pharmaceut Univ, Sch Pharm, Shenyang 110016, Peoples R China; 4.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Div Antitumor Pharmacol, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Chi, Liandi,Wu, Delin,Li, Zhuo,et al. Modified Release and Improved Stability of Unstable BCS II Drug by Using Cyclodextrin Complex as Carrier To Remotely Load Drug into Niosomes[J]. MOLECULAR PHARMACEUTICS,2016,13(1):113-124. |
| APA | Chi, Liandi.,Wu, Delin.,Li, Zhuo.,Zhang, Minmin.,Liu, Hongchun.,...&Zhang, Jiwen.(2016).Modified Release and Improved Stability of Unstable BCS II Drug by Using Cyclodextrin Complex as Carrier To Remotely Load Drug into Niosomes.MOLECULAR PHARMACEUTICS,13(1),113-124. |
| MLA | Chi, Liandi,et al."Modified Release and Improved Stability of Unstable BCS II Drug by Using Cyclodextrin Complex as Carrier To Remotely Load Drug into Niosomes".MOLECULAR PHARMACEUTICS 13.1(2016):113-124. |
入库方式： OAI收割
来源：上海药物研究所
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