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学科主题: 药学
题名:
A Cremophor-Free Self-Microemulsified Delivery System for Intravenous Injection of Teniposide: Evaluation In Vitro and In Vivo
作者: He, Suna1,2; Cui, Zheng2; Mei, Dong2; Zhang, Hua2; Wang, Xueqing2; Dai, Wenbing2; Zhang, Qiang1,2
关键词: characterization ; pharmacokinetics ; self-microemulsified drug delivery system ; teniposide ; tissue distribution
刊名: AAPS PHARMSCITECH
发表日期: 2012-09-01
DOI: 10.1208/s12249-012-9809-0
卷: 13, 期:3, 页:846-852
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]: PHARMACOKINETICS ; FORMULATION ; PACLITAXEL ; NANOPARTICLES ; EMULSION ; VM-26 ; EL ; HYPERSENSITIVITY ; CHEMOTHERAPY ; MALIGNANCIES
英文摘要:

In order to tackle the problems on low water solubility of teniposide, involvement of toxic surfactant in its injection, and the poor stability during infusion, a Cremophor-free teniposide self-microemulsified drug delivery system (TEN-SMEDDS) was prepared for the first time, characterized, and evaluated in comparison with teniposide injection (VUMON) in vitro and in vivo. The optimized formulation contained N, N-dimethylacetamide, medium-chain triglyceride, lecithin, and dehydrated alcohol besides teniposide. The TEN-SMEDDS could form fine droplets with mean diameter of 282 +/- 21 nm and zeta potential of -7.5 +/- 1.7 mV after dilution with 5% glucose, which were stable within 4 h. The release of teniposide from TEN-SMEDDS and VUMON was similar. However, the pharmacokinetic behavior of TEN-SMEDDS in rats was different from that of VUMON, evidenced by the lower area under the concentration-time curve and larger volume of distribution in emulsion group. Finally, TEN-SMEDDS was found to distribute more teniposide in most tissues, especially in reticuloendothelial system, after intravenous administration to rats. Importantly, brain drug level in TEN-SMEDDS group was higher than or similar to that in control group, although the emulsion system had a lower plasma drug concentration. In conclusion, the novel SMEDDS prepared here, without toxic surfactant and as an oil solution before use, may be potential for clinical use due to its low toxicity and high store stability. It may be favorable for the treatment of some tumors like cerebroma, since it may achieve the relatively higher drug level in brain but lower blood concentration.

语种: 英语
所属项目编号: 81130059 ; 2009CB930300 ; BMU20110263
项目资助者: National Nature Science Foundation ; National Basic Research Program of China ; Innovation Team of Ministry of Education
WOS记录号: WOS:000313499300012
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/56966
Appears in Collections:北京大学药学院_期刊论文

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作者单位: 1.Shenyang Pharmaceut Univ, Sch Pharm, Dept Pharmaceut, Shenyang, Peoples R China
2.Peking Univ, Sch Pharmaceut Sci, State Key Lab Nat & Biomimet Drugs, Beijing 100871, Peoples R China

Recommended Citation:
He, Suna,Cui, Zheng,Mei, Dong,et al. A Cremophor-Free Self-Microemulsified Delivery System for Intravenous Injection of Teniposide: Evaluation In Vitro and In Vivo[J]. AAPS PHARMSCITECH,2012,13(3):846-852.
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