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学科主题: 药学
题名:
Preparation, characterization and pharmacokinetics of Amoitone B-loaded long circulating nanostructured lipid carriers
作者: Luan, Jingjing1; Zhang, Dianrui1; Hao, Leilei1; Qi, Lisi1; Liu, Xinquan1; Guo, Hejian1; Li, Caiyun1; Guo, Yuanyuan1; Li, Tingting1; Zhang, Qiang2; Zhai, Guangxi1
关键词: Amoitone B ; Nanostructured lipid carriers ; Long circulation ; In vitro release ; Pharmacokinetics
刊名: COLLOIDS AND SURFACES B-BIOINTERFACES
发表日期: 2014-02-01
DOI: 10.1016/j.colsurfb.2013.10.018
卷: 114, 页:255-260
收录类别: SCI
文章类型: Article
WOS标题词: Science & Technology
类目[WOS]: Biophysics ; Chemistry, Physical ; Materials Science, Biomaterials
研究领域[WOS]: Biophysics ; Chemistry ; Materials Science
关键词[WOS]: ORPHAN NUCLEAR RECEPTORS ; CANCER-CELLS ; DRUG-DELIVERY ; IN-VITRO ; NUR77 ; NANOPARTICLES ; TECHNOLOGY ; PACLITAXEL ; APOPTOSIS ; VIVO
英文摘要:

Amoitone B, chemically synthesized as the derivative of Cytosporone B, is a powerful agonist for Nur77 receptor. It has outstanding anticancer activity in vivo. However, the water-insolubility and short biological half-life lead to poor bioavailability, which limits its application. The aim of this study was to develop polyethylene glycol-coated Amoitone B-loaded nanostructured lipid carriers (AmB-PEG-NLC) for parenteral delivery of Amoitone B to prolong drug circulation time in body and enhance the bioavailability. AmB-PEG-NLC were prepared by emulsion-evaporation and low temperature-solidification method, while Amoitone B-loaded NLC (AmB-NLC) were also prepared as control. The characteristics of AmB-PEG-NLC and AmB-NLC such as particle size, zeta potential, entrapment efficiency and drug loading were investigated in detail. The mean particle size was about 200 nm and the zeta potential value was about - 15 mV. The X-ray diffraction analysis demonstrated that Amoitone B was not in crystalline state in NLC (AmB-PEG-NLC and AmB-NLC). Drug release pattern with burst release initially and prolonged release afterwards was obtained in vitro for AmB-PEG-NLC. Furthermore, AmB-PEG-NLC exhibited prolonged MRT (mean residence time) and higher AUC (area under drug concentration-time curve) compared with AmB-NLC as well as Amoitone B solution. These results indicated that AmB-PEG-NLC could be a promising delivery system for Amoitone B to prolong the circulation time in body and thus improve its bioavailability. (C) 2013 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 (973 Program)
WOS记录号: WOS:000331596100034
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/65262
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, Coll Pharm, Jinan 250012, Peoples R China
2.Peking Univ, Sch Pharmaceut Sci, State Key Lab Nat & Biomimet Drugs, Beijing 100083, Peoples R China

Recommended Citation:
Luan, Jingjing,Zhang, Dianrui,Hao, Leilei,et al. Preparation, characterization and pharmacokinetics of Amoitone B-loaded long circulating nanostructured lipid carriers[J]. COLLOIDS AND SURFACES B-BIOINTERFACES,2014,114:255-260.
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