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Antitumor efficacy of a novel CLA-PTX microemulsion against brain tumors: in vitro and in vivo findings
Li, Dan1; Yang, Ke1; Li, Jie-Si1; Ke, Xi-Yu1; Duan, Yu1; Du, Ruo1; Song, Ping1; Yu, Ke-Fu1; Ren, Wei1; Huang, Dan1; Li, Xing-Huo1; Hu, Xin1; Zhang, Xuan1; Zhang, Qiang1,2
关键词Cla-ptx Microemulsion Pharmacokinetics Brain Tumor Antitumor Efficacy Safety
刊名INTERNATIONAL JOURNAL OF NANOMEDICINE
2012
DOI10.2147/IJN.S38927
7页:6105-6114
收录类别SCI
文章类型Article
WOS标题词Science & Technology
类目[WOS]Nanoscience & Nanotechnology ; Pharmacology & Pharmacy
研究领域[WOS]Science & Technology - Other Topics ; Pharmacology & Pharmacy
关键词[WOS]CONJUGATED LINOLEIC-ACID ; BREAST-CANCER CELLS ; DRUG-DELIVERY SYSTEM ; WATER-SOLUBLE DRUGS ; NANOEMULSION FORMULATIONS ; ORAL BIOAVAILABILITY ; INTRANASAL DELIVERY ; LIPID NANOPARTICLES ; SOLID DISPERSION ; PACLITAXEL
英文摘要

Background: Considering the observations that linoleic acid conjugated with paclitaxel (CLA-PTX) possesses antitumor activity against brain tumors, is able to cross the blood-brain barrier, but has poor water solubility, the purpose of this study was to prepare a novel CLA-PTX microemulsion and evaluate its activity against brain tumors in vitro and in vivo.

Methods: The in vitro cytotoxicity of a CLA-PTX microemulsion was investigated in C6 glioma cells. The in vivo antitumor activity of the CLA-PTX microemulsion was evaluated in tumor-bearing nude mice and rats. The pharmacokinetics of the CLA-PTX microemulsion were investigated in rats, and its safety was also evaluated in mice.

Results: The average droplet size of the CLA-PTX microemulsion was approximately 176.3 +/- 0.8 nm and the polydispersity index was 0.294 +/- 0.024. In vitro cytotoxicity results showed that the IC50 of the CLA-PTX microemulsion was 1.61 +/- 0.83 mu M for a C6 glioma cell line, which was similar to that of free paclitaxel and CLA-PTX solution (P > 0.05). The antitumor activity of the CLA-PTX microemulsion against brain tumors was confirmed in our in vivo C6 glioma tumor-bearing nude mice as well as in a rat model. In contrast, Taxol (R) had almost no significant antitumor effect in C6 glioma tumor-bearing rats, but could markedly inhibit growth of C6 tumors in C6 glioma tumor-bearing nude mice. The pharmacokinetic results indicated that CLA-PTX in solution has a much longer circulation time and produces higher drug plasma concentrations compared with the CLA-PTX microemulsion. The results of the acute toxicity study showed that the LD50 of CLA-PTX solution was 103.9 mg/kg. In contrast, the CLA-PTX microemulsion was well tolerated in mice when administered at doses up to 200 mg/kg.

Conclusion: CLA-PTX microemulsion is a novel formulation with significant antitumor efficacy in the treatment of brain tumors, and is safer than CLA-PTX solution.

语种英语
WOS记录号WOS:000312294000001
项目编号81172992 ; 2009CB930300 ; 2013CB932501 ; BMU20110263
资助机构National Natural Science Foundation of China ; National Basic Research Program of China (973 Program) ; Innovation Team of the Ministry of Education
引用统计
被引频次:9[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/400002259/60069
专题北京大学药学院_药剂学系
北京大学药学院
作者单位1.Peking Univ, Sch Pharmaceut Sci, Dept Pharmaceut, Beijing 100191, Peoples R China
2.Peking Univ, Sch Pharmaceut Sci, State Key Lab Nat & Biomimet Drugs, Beijing 100191, Peoples R China
推荐引用方式
GB/T 7714
Li, Dan,Yang, Ke,Li, Jie-Si,et al. Antitumor efficacy of a novel CLA-PTX microemulsion against brain tumors: in vitro and in vivo findings[J]. INTERNATIONAL JOURNAL OF NANOMEDICINE,2012,7:6105-6114.
APA Li, Dan.,Yang, Ke.,Li, Jie-Si.,Ke, Xi-Yu.,Duan, Yu.,...&Zhang, Qiang.(2012).Antitumor efficacy of a novel CLA-PTX microemulsion against brain tumors: in vitro and in vivo findings.INTERNATIONAL JOURNAL OF NANOMEDICINE,7,6105-6114.
MLA Li, Dan,et al."Antitumor efficacy of a novel CLA-PTX microemulsion against brain tumors: in vitro and in vivo findings".INTERNATIONAL JOURNAL OF NANOMEDICINE 7(2012):6105-6114.
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