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学科主题: 药学
题名:
A pegylated liposomal platform: Pharmacokinetics, pharmacodynamics, and toxicity in mice using doxorubicin as a model drug
作者: Lu, WL; Qi, XR; Zhang, Q; Li, RY; Wang, GL; Zhang, RJ; Wei, SL
关键词: pegylated liposomal platform ; doxorubicin ; pharmacokinetics ; pharmacodynamics ; toxicity
刊名: JOURNAL OF PHARMACOLOGICAL SCIENCES
发表日期: 2004-07-01
卷: 95, 期:3, 页:381-389
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]: SOLID TUMORS ; CARCINOMA ; EFFICACY ; METABOLITES ; MURINE
英文摘要:

Aims were to observe pharmacokinetics, pharmacodynamics, and toxicity for constructing a Sino-pegylated liposomal platform. Human hepatocarcinoma cells (Bel7402) and murine hepatocarcinoma cells (H-22) were used for the cytotoxicity assay and the in vivo solid xenograft tumor model in mice, respectively. Pharmacokinetic results in mice showed that the pegylated liposomal doxorubicin markedly prolonged the blood circulation of doxorubicin. Elimination half-time (T-1/2,T-gamma) of pegylated, regular liposomal doxorubicin and free doxorubicin were 46.09 +/- 14.44, 26.04 +/- 3.34, and 23.72 +/- 5.13 h, respectively. The area under the concentration-time curves (AUC(0-infinity)) (h(.)mug/g) of the pegylated and regular liposomal doxorubicin were 6.8- and 2.6-fold higher than that of free doxorubicin, respectively. Cytotoxicity and antitumor activity in vivo indicated that activity of the pegylated liposomal doxorubicin was higher than that of the regular or the free one, respectively. After two weeks of tail intravenous injection of the pegylated liposomal doxorubicin at a single dose of 10 mg/kg, no significant damage was observed in gastric, intestinal mucosa, and heart muscle, but pronounced damages were found in the control group after dosing free doxorubicin. The results demonstrate that the pegylated liposomes improve the efficacy of toxics and reduce the toxicity, therefore providing favorable evidence for building a pegylated liposomal platform.

语种: 英语
WOS记录号: WOS:000222877100012
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/59660
Appears in Collections:北京大学药学院_药剂学系_期刊论文

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作者单位: Peking Univ, Sch Pharmaceut Sci, Dept Pharmaceut, Beijing 100083, Peoples R China

Recommended Citation:
Lu, WL,Qi, XR,Zhang, Q,et al. A pegylated liposomal platform: Pharmacokinetics, pharmacodynamics, and toxicity in mice using doxorubicin as a model drug[J]. JOURNAL OF PHARMACOLOGICAL SCIENCES,2004,95(3):381-389.
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