IR@PKUHSC  > 北京大学药学院
学科主题药学
A Cremophor-Free Self-Microemulsified Delivery System for Intravenous Injection of Teniposide: Evaluation In Vitro and In Vivo
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
2012-09-01
DOI10.1208/s12249-012-9809-0
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
WOS记录号WOS:000313499300012
项目编号81130059 ; 2009CB930300 ; BMU20110263
资助机构National Nature Science Foundation ; National Basic Research Program of China ; Innovation Team of Ministry of Education
引用统计
被引频次:11[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/400002259/56966
专题北京大学药学院
北京大学药学院_药剂学系
北京大学第二临床医学院_药剂科
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
推荐引用方式
GB/T 7714
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.
APA He, Suna.,Cui, Zheng.,Mei, Dong.,Zhang, Hua.,Wang, Xueqing.,...&Zhang, Qiang.(2012).A Cremophor-Free Self-Microemulsified Delivery System for Intravenous Injection of Teniposide: Evaluation In Vitro and In Vivo.AAPS PHARMSCITECH,13(3),846-852.
MLA He, Suna,et al."A Cremophor-Free Self-Microemulsified Delivery System for Intravenous Injection of Teniposide: Evaluation In Vitro and In Vivo".AAPS PHARMSCITECH 13.3(2012):846-852.
条目包含的文件
条目无相关文件。
个性服务
推荐该条目
保存到收藏夹
查看访问统计
导出为Endnote文件
谷歌学术
谷歌学术中相似的文章
[He, Suna]的文章
[Cui, Zheng]的文章
[Mei, Dong]的文章
百度学术
百度学术中相似的文章
[He, Suna]的文章
[Cui, Zheng]的文章
[Mei, Dong]的文章
必应学术
必应学术中相似的文章
[He, Suna]的文章
[Cui, Zheng]的文章
[Mei, Dong]的文章
相关权益政策
暂无数据
收藏/分享
所有评论 (0)
暂无评论
 

除非特别说明,本系统中所有内容都受版权保护,并保留所有权利。