Development and optimization of a self-microemulsifying drug delivery system for atorvastatin calcium by using D-optimal mixture design

Development and optimization of a self-microemulsifying drug delivery system for atorvastatin calcium by using D-optimal mixture design

Dong Woo Yeom,1 Ye Seul Song,1 Sung Rae Kim,1 Sang Gon Lee,1 Min Hyung Kang,1 Sangkil Lee,2 Young Wook Choi1 1College of Pharmacy, Chung-Ang University, Seoul, 2College of Pharmacy, Keimyung University, Daegu, Republic of Korea Abstract: In this study, we developed and optimized a self-microemulsi...

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Autores principales: Yeom DW, Song YS, Kim SR, Lee SG, Kang MH, Lee S, Choi YW
Formato: article
Lenguaje:EN
Publicado: Dove Medical Press 2015
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Medicine (General)
R5-920
Acceso en línea:https://doaj.org/article/8f9ba7731c6d437d9ad97618fcaedeb5
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spelling oai:doaj.org-article:8f9ba7731c6d437d9ad97618fcaedeb52021-12-02T05:02:15ZDevelopment and optimization of a self-microemulsifying drug delivery system for atorvastatin calcium by using D-optimal mixture design1178-2013https://doaj.org/article/8f9ba7731c6d437d9ad97618fcaedeb52015-06-01T00:00:00Zhttp://www.dovepress.com/development-and-optimization-of-a-self-microemulsifying-drug-delivery--peer-reviewed-article-IJNhttps://doaj.org/toc/1178-2013Dong Woo Yeom,1 Ye Seul Song,1 Sung Rae Kim,1 Sang Gon Lee,1 Min Hyung Kang,1 Sangkil Lee,2 Young Wook Choi1 1College of Pharmacy, Chung-Ang University, Seoul, 2College of Pharmacy, Keimyung University, Daegu, Republic of Korea Abstract: In this study, we developed and optimized a self-microemulsifying drug delivery system (SMEDDS) formulation for improving the dissolution and oral absorption of atorvastatin calcium (ATV), a poorly water-soluble drug. Solubility and emulsification tests were performed to select a suitable combination of oil, surfactant, and cosurfactant. A d-optimal mixture design was used to optimize the concentration of components used in the SMEDDS formulation for achieving excellent physicochemical characteristics, such as small droplet size and high dissolution. The optimized ATV-loaded SMEDDS formulation containing 7.16% Capmul MCM (oil), 48.25% Tween 20 (surfactant), and 44.59% Tetraglycol (cosurfactant) significantly enhanced the dissolution rate of ATV in different types of medium, including simulated intestinal fluid, simulated gastric fluid, and distilled water, compared with ATV suspension. Good agreement was observed between predicted and experimental values for mean droplet size and percentage of the drug released in 15 minutes. Further, pharmacokinetic studies in rats showed that the optimized SMEDDS formulation considerably enhanced the oral absorption of ATV, with 3.4-fold and 4.3-fold increases in the area under the concentration-time curve and time taken to reach peak plasma concentration, respectively, when compared with the ATV suspension. Thus, we successfully developed an optimized ATV-loaded SMEDDS formulation by using the d-optimal mixture design, that could potentially be used for improving the oral absorption of poorly water-soluble drugs. Keywords: atorvastatin, SMEDDS, d-optimal mixture design, optimization, dissolution, bioavailability Yeom DWSong YSKim SRLee SGKang MHLee SChoi YWDove Medical PressarticleMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol 2015, Iss default, Pp 3865-3878 (2015)
institution DOAJ
collection DOAJ
language EN
topic Medicine (General)
R5-920
spellingShingle Medicine (General)
R5-920
Yeom DW
Song YS
Kim SR
Lee SG
Kang MH
Lee S
Choi YW
Development and optimization of a self-microemulsifying drug delivery system for atorvastatin calcium by using D-optimal mixture design
description Dong Woo Yeom,1 Ye Seul Song,1 Sung Rae Kim,1 Sang Gon Lee,1 Min Hyung Kang,1 Sangkil Lee,2 Young Wook Choi1 1College of Pharmacy, Chung-Ang University, Seoul, 2College of Pharmacy, Keimyung University, Daegu, Republic of Korea Abstract: In this study, we developed and optimized a self-microemulsifying drug delivery system (SMEDDS) formulation for improving the dissolution and oral absorption of atorvastatin calcium (ATV), a poorly water-soluble drug. Solubility and emulsification tests were performed to select a suitable combination of oil, surfactant, and cosurfactant. A d-optimal mixture design was used to optimize the concentration of components used in the SMEDDS formulation for achieving excellent physicochemical characteristics, such as small droplet size and high dissolution. The optimized ATV-loaded SMEDDS formulation containing 7.16% Capmul MCM (oil), 48.25% Tween 20 (surfactant), and 44.59% Tetraglycol (cosurfactant) significantly enhanced the dissolution rate of ATV in different types of medium, including simulated intestinal fluid, simulated gastric fluid, and distilled water, compared with ATV suspension. Good agreement was observed between predicted and experimental values for mean droplet size and percentage of the drug released in 15 minutes. Further, pharmacokinetic studies in rats showed that the optimized SMEDDS formulation considerably enhanced the oral absorption of ATV, with 3.4-fold and 4.3-fold increases in the area under the concentration-time curve and time taken to reach peak plasma concentration, respectively, when compared with the ATV suspension. Thus, we successfully developed an optimized ATV-loaded SMEDDS formulation by using the d-optimal mixture design, that could potentially be used for improving the oral absorption of poorly water-soluble drugs. Keywords: atorvastatin, SMEDDS, d-optimal mixture design, optimization, dissolution, bioavailability 
format article
author Yeom DW
Song YS
Kim SR
Lee SG
Kang MH
Lee S
Choi YW
author_facet Yeom DW
Song YS
Kim SR
Lee SG
Kang MH
Lee S
Choi YW
author_sort Yeom DW
title Development and optimization of a self-microemulsifying drug delivery system for atorvastatin calcium by using D-optimal mixture design
title_short Development and optimization of a self-microemulsifying drug delivery system for atorvastatin calcium by using D-optimal mixture design
title_full Development and optimization of a self-microemulsifying drug delivery system for atorvastatin calcium by using D-optimal mixture design
title_fullStr Development and optimization of a self-microemulsifying drug delivery system for atorvastatin calcium by using D-optimal mixture design
title_full_unstemmed Development and optimization of a self-microemulsifying drug delivery system for atorvastatin calcium by using D-optimal mixture design
title_sort development and optimization of a self-microemulsifying drug delivery system for atorvastatin calcium by using d-optimal mixture design
publisher Dove Medical Press
publishDate 2015
url https://doaj.org/article/8f9ba7731c6d437d9ad97618fcaedeb5
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