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An oil-free microemulsion for intravenous delivery of diallyl trisulfide: Formulation and evaluation
Li, Xinru1; Yue, Yuanting1; Zhou, Yanxia1; Fan, Yating1; Fan, Chao1; Huang, Yanqing2; Wu, Fei1; Liu, Yan1
关键词Diallyl trisulfide Microemulsion Safety Pharmacokinetics
刊名INTERNATIONAL JOURNAL OF PHARMACEUTICS
2011-04-04
DOI10.1016/j.ijpharm.2011.01.008
407期:1-2页:158-166
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]ALLYL SULFUR-COMPOUNDS ; PROSTATE-CANCER CELLS ; GARLIC OIL ; IN-VITRO ; ORGANOSULFUR COMPOUNDS ; INTRANASAL DELIVERY ; MEDIATED APOPTOSIS ; CREMOPHOR EL ; PACLITAXEL ; SYSTEM
英文摘要

The aim of the present study was to develop an oil-free o/w microemulsion, Cremophor EL:ethanol-propylene glycol:saline, for diallyl trisulfide (OATS) for intravenous (i.v.) administration to modify the safety and pharmacokinetics of OATS. The ternary diagram was constructed to identify the regions of dilutable microemulsions, and the optimal composition of microemulsion was determined by evaluation of injection safety such as hemolysis, intravenous stimulation and injection anaphylaxis compared to commercial formulation Chentian (R). Promising microemulsion with modified injection safety was developed that could incorporate 100 mg/g of DATS. The droplet size of the microemulsion was about 26 nm in diameter with narrow distribution (polydispersity index: 0.14). Acute toxicity test showed that median lethal dose (LD(50)) of DATS microemulsion was 1.69-fold higher than that of Chentian (R). Pharmacokinetics was assessed by comparing with the commercial injection after intravenous administration to rats at a dose of 30 mg/kg. The developed microemulsion showed significant higher area under the drug concentration-time curve and lower clearance and distribution volume than those of Chentian (R) (p<0.05). This helped DATS to reach higher level in vessel, and circulate in the blood stream for a longer time resulting in better therapeutic effect. In conclusion, microemulsion would be a promising intravenous delivery system for DATS. (C) 2011 Elsevier BM. All rights reserved.

语种英语
WOS记录号WOS:000288777400020
项目编号2009zx09310-001 ; 2009CB930300
资助机构National Development of Significant New Drugs (New Preparation and New Technology) ; National Basic Research Program of China (973 program)
引用统计
被引频次:15[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/400002259/59023
专题北京大学药学院_药剂学系
作者单位1.Peking Univ, Sch Pharmaceut Sci, Dept Pharmaceut, Beijing 100191, Peoples R China
2.Peking Univ, Sch Pharmaceut Sci, Pharmaceut Teaching Expt Ctr, Beijing 100191, Peoples R China
推荐引用方式
GB/T 7714
Li, Xinru,Yue, Yuanting,Zhou, Yanxia,et al. An oil-free microemulsion for intravenous delivery of diallyl trisulfide: Formulation and evaluation[J]. INTERNATIONAL JOURNAL OF PHARMACEUTICS,2011,407(1-2):158-166.
APA Li, Xinru.,Yue, Yuanting.,Zhou, Yanxia.,Fan, Yating.,Fan, Chao.,...&Liu, Yan.(2011).An oil-free microemulsion for intravenous delivery of diallyl trisulfide: Formulation and evaluation.INTERNATIONAL JOURNAL OF PHARMACEUTICS,407(1-2),158-166.
MLA Li, Xinru,et al."An oil-free microemulsion for intravenous delivery of diallyl trisulfide: Formulation and evaluation".INTERNATIONAL JOURNAL OF PHARMACEUTICS 407.1-2(2011):158-166.
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