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学科主题药学
Epirubicin-encapsulated long-circulating thermosensitive liposome improves pharmacokinetics and antitumor therapeutic efficacy in animals
Wu, Yan1,5; Yang, Yuan2,5; Zhang, Fu-Cheng1; Wu, Cheng3,5; Lue, Wan-Liang4; Mei, Xing-Guo5
关键词Thermosensitive Liposome Pharmacokinetics Epirubicin Hydrochloride Antitumor
刊名JOURNAL OF LIPOSOME RESEARCH
2011-09-01
DOI10.3109/08982104.2010.520273
21期:3页:221-228
收录类别SCI
文章类型Article
WOS标题词Science & Technology
类目[WOS]Biochemistry & Molecular Biology ; Pharmacology & Pharmacy
资助者National Natural Science Foundation of China ; National Natural Science Foundation of China
研究领域[WOS]Biochemistry & Molecular Biology ; Pharmacology & Pharmacy
关键词[WOS]TUMOR XENOGRAFT MODEL ; HIGH-DOSE EPIRUBICIN ; DRUG-RELEASE ; DOXORUBICIN ; DELIVERY ; HYPERTHERMIA ; STABILITY ; PLASMA
英文摘要

In the present work, a long-circulating epirubicin hydrochloride (EPI)-containing thermosensitive liposome aiming at antitumor therapy, DPPC/MSPC/DSPG/DSPE-mPEG(2000) (EPI-LTSL), was developed and evaluated. Nonthermosensitive and traditional liposomes, HSPC/cholesterol/DSPG/DSPE-mPEG(2000) (EPI-NTSL) and HSPC/cholesterol (EPI-LIP), were also prepared at the same time for comparison. Temperature-dependent EPI release from loaded liposomes in vitro was characterized by the fluorescence method. Different liposome preparations were administered in rats by intravenous injection at the same dosage of 12 mg.kg(-1). EPI and internal standard daunorubicin hydrochloride (DAU) were analyzed by high-performance liquid chromatography and verified by LC tandem mass spectrometry. In the pharmacodynamics study, the EPI-LTSL was combined with local hyperthermia for target-specific delivery to the anesthetized and tumor-bearing mice. According to the in vitro results, more than 90% of loaded EPI was released from MSPC-containing liposome (EPI-LTSL) within 4 minutes at 43 degrees C, while at 37 degrees C, less than 5% was released beyond 60 minutes. However, less than 5% of drug was released at 43 degrees C for the other two liposomes without MSPC (EPI-NTSL and EPI-LIP). The results of the pharmacokinetics study in rats showed that not only the circulation time of EPI was prolonged significantly, but also the concentration in vivo was promoted for EPI-LTSL, compared to EPI-NTSL and EPI-solution. The mean tumor inhibitory rate for EPI-LTSL, EPI-NTSL, and EPI-solution were 61.1, 39.6, and 43.1%, respectively.

语种英语
所属项目编号30901870 ; 2007CB935801
资助者National Natural Science Foundation of China ; National Natural Science Foundation of China
WOS记录号WOS:000293915600005
Citation statistics
Cited Times:11[WOS]   [WOS Record]     [Related Records in WOS]
文献类型期刊论文
条目标识符http://ir.bjmu.edu.cn/handle/400002259/52980
Collection北京大学药学院
作者单位1.Gen Hosp Second Artillery, Dept Pharm, Beijing, Peoples R China
2.Peking Univ, Sch Pharm, Beijing 100871, Peoples R China
3.Gen Hosp Air Force, Dept Pharm, Beijing, Peoples R China
4.Beijing Acad Agr & Forestry Sci, Inst Forestry & Pomol, Beijing, Peoples R China
5.Beijing Inst Pharmacol & Toxicol, Beijing, Peoples R China
Recommended Citation
GB/T 7714
Wu, Yan,Yang, Yuan,Zhang, Fu-Cheng,et al. Epirubicin-encapsulated long-circulating thermosensitive liposome improves pharmacokinetics and antitumor therapeutic efficacy in animals[J]. JOURNAL OF LIPOSOME RESEARCH,2011,21(3):221-228.
APA Wu, Yan,Yang, Yuan,Zhang, Fu-Cheng,Wu, Cheng,Lue, Wan-Liang,&Mei, Xing-Guo.(2011).Epirubicin-encapsulated long-circulating thermosensitive liposome improves pharmacokinetics and antitumor therapeutic efficacy in animals.JOURNAL OF LIPOSOME RESEARCH,21(3),221-228.
MLA Wu, Yan,et al."Epirubicin-encapsulated long-circulating thermosensitive liposome improves pharmacokinetics and antitumor therapeutic efficacy in animals".JOURNAL OF LIPOSOME RESEARCH 21.3(2011):221-228.
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