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学科主题药学
Nimodipine-loaded mixed micelles: formulation, compatibility, pharmacokinetics, and vascular irritability study
Song, Xu1; Jiang, Yu2; Ren, Chunjuan1; Sun, Xun1; Zhang, Qiang3; Gong, Tao1; Zhang, Zhirong1
关键词drug loading nimodipine injection physical compatibility solubilizing efficiency
刊名INTERNATIONAL JOURNAL OF NANOMEDICINE
2012
DOI10.2147/IJN.S33228
7页:3689-3699
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]BILE-SALT ; CEREBROVASCULAR-DISEASE ; DRUG SOLUBILITY ; ISCHEMIC STROKE ; PHOSPHATIDYLCHOLINE ; STABILITY ; LECITHIN ; DELIVERY
英文摘要

Background: The clinical application of nimodipine (NIM) is limited by several unfavorable properties, which are induced by its low aqueous solubility. In the present study, nimodipine-loaded egg phosphatidylcholine-sodium glycocholate mixed micelles (NIM-EPC-SGC-MMs) were prepared to improve the water solubility of NIM, thus allowing it to be more applicable for clinical use.

Methods: NIM-EPC-SGC-MMs were prepared using the coprecipitation method and the factors influencing formulation quality were optimized. After formulation, water solubility, solubilizing efficiency, drug loading, particle size, physical compatibility, pharmacokinetics, and vascular irritability were determined.

Results: The mean size of the NIM-EPC-SGC-MMs was 6.099 +/- 0.048 nm under optimized conditions. The water solubility of NIM in EPC-SGC-MMs was enhanced 250-fold compared with free NIM. The physical compatibility, pharmacokinetic, and vascular irritability studies showed that, in comparison to the commercially available NIM injections, NIM-EPC-SGC-MMs presented better physical compatibility, the same pharmacokinetic profile, and less risk of local vascular irritation and phlebitis.

Conclusion: EPC-SGC-MMs represent a promising new formulation suitable for the intravenous delivery of NIM.

语种英语
WOS记录号WOS:000306507100001
项目编号2009CB930300 ; 2011ZX09501-001-01
资助机构National Basic Research Program of China (973 program) ; National S and T Major Project of China
引用统计
被引频次:13[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/400002259/65296
专题北京大学药学院
北京大学第三临床医学院_骨科
作者单位1.Sichuan Univ, Minist Educ, Key Lab Drug Targeting & Drug Delivery Syst, W China Sch Pharm, Chengdu 610041, Peoples R China
2.Peking Univ, Ctr Drug Evaluat State Food & Drug Adm, Beijing, Peoples R China
3.Peking Univ, Sch Pharmaceut Sci, State Key Lab Nat & Biomimet Drugs, Beijing, Peoples R China
推荐引用方式
GB/T 7714
Song, Xu,Jiang, Yu,Ren, Chunjuan,et al. Nimodipine-loaded mixed micelles: formulation, compatibility, pharmacokinetics, and vascular irritability study[J]. INTERNATIONAL JOURNAL OF NANOMEDICINE,2012,7:3689-3699.
APA Song, Xu.,Jiang, Yu.,Ren, Chunjuan.,Sun, Xun.,Zhang, Qiang.,...&Zhang, Zhirong.(2012).Nimodipine-loaded mixed micelles: formulation, compatibility, pharmacokinetics, and vascular irritability study.INTERNATIONAL JOURNAL OF NANOMEDICINE,7,3689-3699.
MLA Song, Xu,et al."Nimodipine-loaded mixed micelles: formulation, compatibility, pharmacokinetics, and vascular irritability study".INTERNATIONAL JOURNAL OF NANOMEDICINE 7(2012):3689-3699.
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