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Synthesis, characterization, in vitro and in vivo evaluation of PEGylated oridonin conjugates
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
2013-11-01
DOI10.1016/j.ijpharm.2013.08.014
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
WOS记录号WOS:000324523400010
项目编号2009CB930300
资助机构National Basic Research Program of China (973 Program)
引用统计
被引频次:17[WOS]   [WOS记录]     [WOS相关记录]
文献类型期刊论文
条目标识符http://ir.bjmu.edu.cn/handle/400002259/59488
专题北京大学药学院
北京大学药学院_药剂学系
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
推荐引用方式
GB/T 7714
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.
APA Shen, Jingyi.,Zhang, Dianrui.,Zhao, Zhongxi.,Jia, Lejiao.,Zheng, Dandan.,...&Guo, Hejian.(2013).Synthesis, characterization, in vitro and in vivo evaluation of PEGylated oridonin conjugates.INTERNATIONAL JOURNAL OF PHARMACEUTICS,456(1),80-86.
MLA Shen, Jingyi,et al."Synthesis, characterization, in vitro and in vivo evaluation of PEGylated oridonin conjugates".INTERNATIONAL JOURNAL OF PHARMACEUTICS 456.1(2013):80-86.
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