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学科主题: 药学
题名:
Synthesis, characterization, in vitro and in vivo evaluation of PEGylated oridonin conjugates
作者: Shen, Jingyi1; Zhang, Dianrui1; Zhao, Zhongxi2,3; Jia, Lejiao1; Zheng, Dandan1; Liu, Guangpu1; Hao, Leilei1; Zhang, Qiang4; Tian, Xiaona1; Li, Caiyun1; Guo, Hejian1
关键词: Oridonin ; Poly(ethylene glycol) ; Conjugation ; Synthesis ; Drug delivery systems ; Pharmacokinetics
刊名: INTERNATIONAL JOURNAL OF PHARMACEUTICS
发表日期: 2013-11-01
DOI: 10.1016/j.ijpharm.2013.08.014
卷: 456, 期:1, 页:80-86
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]: NANOSTRUCTURED LIPID CARRIERS ; ANTITUMOR-ACTIVITY ; POLY(ETHYLENE GLYCOL) ; DRUG-DELIVERY ; DERIVATIVES ; PRODRUGS ; CELLS ; TAXOL
英文摘要:

Oridonin (ORI), a diterpenoid compound with promising antitumor activity, was proved to possess potent antileukemia efficacies in vitro and in vivo recently. However, the development and application of ORI was limited by its poor solubility and rapid plasma clearance. The purpose of this study was to solve these problems. PEGylated oridonin linked with succinic acid (SA) as spacer moiety (PEG-SA-ORI conjugate) was synthesized. mPEG amines with four specifications of molecular weight (MW) were utilized. All polymeric conjugates showed satisfactory aqueous solubility and in vitro studies implied that the drug solubility and release features of conjugates were relevant to PEGs. The drug solubility increased more when the MW of PEG was lower, while more significant sustained-release effect was shown with higher PEG MW. Moreover, the release behaviors of conjugates showed a pH-sensitive property. In vivo pharmacokinetic studies demonstrated that the elimination half-life was prolonged in comparison with ORI solution. PEGylation could be a promising method to obtain better efficacy in the field of drug delivery system. (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:000324523400010
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/59488
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, Dept Pharmaceut, Jinan 250012, Peoples R China
2.Shandong Univ, Sch Pharmaceut Sci, Jinan 250012, Peoples R China
3.Shandong Univ, Ctr Pharmaceut Res & Drug Delivery Syst, Jinan 250012, Peoples R China
4.Peking Univ, Sch Pharmaceut Sci, State Key Lab Nat & Biomimet Drugs, Beijing 100083, Peoples R China

Recommended Citation:
Shen, Jingyi,Zhang, Dianrui,Zhao, Zhongxi,et al. Synthesis, characterization, in vitro and in vivo evaluation of PEGylated oridonin conjugates[J]. INTERNATIONAL JOURNAL OF PHARMACEUTICS,2013,456(1):80-86.
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