Nimodipine-loaded mixed micelles: formulation, compatibility, pharmacokinetics, and vascular irritability study

Xu Song,1* Yu Jiang,2* Chunjuan Ren,1 Xun Sun,1 Qiang Zhang,3 Tao Gong,1 Zhirong Zhang1 1Key Laboratory of Drug Targeting and Drug Delivery System, Ministry of Education, West China School of Pharmacy, Sichuan University, Chengdu, 2Center for Drug Evaluation, State Food and Drug Administration, 3Sta...

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Autores principales:	Song X, Jiang Y, Ren CJ, Sun X, Zhang Q, Gong T, Zhang ZR
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2012
Materias:	Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/241aa6f475424a9ca73e60787168128a
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spelling	oai:doaj.org-article:241aa6f475424a9ca73e60787168128a2021-12-02T00:43:24ZNimodipine-loaded mixed micelles: formulation, compatibility, pharmacokinetics, and vascular irritability study1176-91141178-2013https://doaj.org/article/241aa6f475424a9ca73e60787168128a2012-07-01T00:00:00Zhttp://www.dovepress.com/nimodipine-loaded-mixed-micelles-formulation-compatibility-pharmacokin-a10394https://doaj.org/toc/1176-9114https://doaj.org/toc/1178-2013Xu Song,1* Yu Jiang,2* Chunjuan Ren,1 Xun Sun,1 Qiang Zhang,3 Tao Gong,1 Zhirong Zhang1 1Key Laboratory of Drug Targeting and Drug Delivery System, Ministry of Education, West China School of Pharmacy, Sichuan University, Chengdu, 2Center for Drug Evaluation, State Food and Drug Administration, 3State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University, Peking, People&#39;s Republic of China*These authors contributed equally to this workBackground: 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 &plusmn; 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.Keywords: drug loading, nimodipine injection, physical compatibility, solubilizing efficiencySong XJiang YRen CJSun XZhang QGong TZhang ZRDove Medical PressarticleMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol 2012, Iss default, Pp 3689-3699 (2012)
institution	DOAJ
collection	DOAJ
language	EN
topic	Medicine (General) R5-920
spellingShingle	Medicine (General) R5-920 Song X Jiang Y Ren CJ Sun X Zhang Q Gong T Zhang ZR Nimodipine-loaded mixed micelles: formulation, compatibility, pharmacokinetics, and vascular irritability study
description	Xu Song,1* Yu Jiang,2* Chunjuan Ren,1 Xun Sun,1 Qiang Zhang,3 Tao Gong,1 Zhirong Zhang1 1Key Laboratory of Drug Targeting and Drug Delivery System, Ministry of Education, West China School of Pharmacy, Sichuan University, Chengdu, 2Center for Drug Evaluation, State Food and Drug Administration, 3State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University, Peking, People&#39;s Republic of China*These authors contributed equally to this workBackground: 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 &plusmn; 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.Keywords: drug loading, nimodipine injection, physical compatibility, solubilizing efficiency
format	article
author	Song X Jiang Y Ren CJ Sun X Zhang Q Gong T Zhang ZR
author_facet	Song X Jiang Y Ren CJ Sun X Zhang Q Gong T Zhang ZR
author_sort	Song X
title	Nimodipine-loaded mixed micelles: formulation, compatibility, pharmacokinetics, and vascular irritability study
title_short	Nimodipine-loaded mixed micelles: formulation, compatibility, pharmacokinetics, and vascular irritability study
title_full	Nimodipine-loaded mixed micelles: formulation, compatibility, pharmacokinetics, and vascular irritability study
title_fullStr	Nimodipine-loaded mixed micelles: formulation, compatibility, pharmacokinetics, and vascular irritability study
title_full_unstemmed	Nimodipine-loaded mixed micelles: formulation, compatibility, pharmacokinetics, and vascular irritability study
title_sort	nimodipine-loaded mixed micelles: formulation, compatibility, pharmacokinetics, and vascular irritability study
publisher	Dove Medical Press
publishDate	2012
url	https://doaj.org/article/241aa6f475424a9ca73e60787168128a
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Nimodipine-loaded mixed micelles: formulation, compatibility, pharmacokinetics, and vascular irritability study

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