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学科主题: 药学
题名:
Studies on the preparation, characterization and pharmacokinetics of Amoitone B nanocrystals
作者: Hao, Leilei1; Wang, Xiaoyong2; Zhang, Dianrui1; Xu, Qingyan2; Song, Siyang2; Wang, Feihu1; Li, Caiyun1; Guo, Hejian1; Liu, Yue1; Zheng, Dandan1; Zhang, Qiang3
关键词: Amoitone B ; Nanocrystals ; Microfluidization method ; In vitro dissolution ; Pharmacokinetics
刊名: INTERNATIONAL JOURNAL OF PHARMACEUTICS
发表日期: 2012-08-20
DOI: 10.1016/j.ijpharm.2012.05.002
卷: 433, 期:1-2, 页:157-164
收录类别: SCI
文章类型: Article
WOS标题词: Science & Technology
类目[WOS]: Pharmacology & Pharmacy
研究领域[WOS]: Pharmacology & Pharmacy
关键词[WOS]: POORLY SOLUBLE DRUGS ; ORPHAN-RECEPTOR NUR77 ; CANCER CELLS ; TISSUE DISTRIBUTION ; ORAL BIOAVAILABILITY ; PROAPOPTOTIC GENES ; NUCLEAR RECEPTORS ; DELIVERY-SYSTEM ; PARTICLE-SIZE ; IN-VIVO
英文摘要:

Amoitone B, as a new derivative of cytosporone B, has been proved to be a natural agonist for Nur77. It exhibits remarkable anticancer activity in vivo and has the potential to be a therapeutic agent for cancer treatment. However, the poor solubility and dissolution rate result in low therapeutic index for injection and low bioavailability for oral administration, therefore limiting its application. In order to magnify the clinical use of Amoitone B, nanocrystal was selected as an application technology to solve the above problems. In this study, the optimized Amoitone B nanocrystals with small and uniform particle size were successfully prepared by microfluidization method and investigated by morphology, size distribution, and zeta potential. The differential scanning calorimetry (DSC) and X-ray diffraction (XRD) confirmed there was no crystalline state changed in the size reduction process. For Amoitone B nanocrystals, an accelerated dissolution velocity and increased saturation solubility were achieved in vitro and a markedly different pharmacokinetic property in vivo was exhibited with retarded clearance and magnified AUC compared with Amoitone B solution. These results implied that developing Amoitone B as nanocrystals is a promising choice for intravenous delivery and further application for cancer therapy. (C) 2012 Elsevier B. V. All rights reserved.

语种: 英语
所属项目编号: 2009CB930300
项目资助者: National Basic Research Program of China (973Program)
WOS记录号: WOS:000305420100020
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/50464
Appears in Collections:北京大学药学院_期刊论文

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作者单位: 1.Shandong Univ, Dept Pharmaceut, Coll Pharm, Jinan 250012, Peoples R China
2.Xiamen Univ, State Key Lab Stress Cellular Biol, Sch Life Sci, Xiamen 361005, Fujian, Peoples R China
3.Peking Univ, State Key Lab Nat & Biomimet Drugs, Sch Pharmaceut Sci, Beijing 100083, Peoples R China

Recommended Citation:
Hao, Leilei,Wang, Xiaoyong,Zhang, Dianrui,et al. Studies on the preparation, characterization and pharmacokinetics of Amoitone B nanocrystals[J]. INTERNATIONAL JOURNAL OF PHARMACEUTICS,2012,433(1-2):157-164.
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