Enhanced oral bioavailability of valsartan using a polymer-based supersaturable self-microemulsifying drug delivery system
Dong Woo Yeom,1,* Bo Ram Chae,2,* Ho Yong Son,1 Jin Han Kim,1 Jun Soo Chae,1 Seh Hyon Song,2 Dongho Oh,2 Young Wook Choi1 1College of Pharmacy, Chung-Ang University, Seoul, 2Daewon Pharm. Co., Ltd, Seoul, Republic of Korea *These authors contributed equally to this work Abstract: A novel, supersa...
Guardado en:
Autores principales: | , , , , , , , |
---|---|
Formato: | article |
Lenguaje: | EN |
Publicado: |
Dove Medical Press
2017
|
Materias: | |
Acceso en línea: | https://doaj.org/article/85d1410562734444aea958f3485cbe53 |
Etiquetas: |
Agregar Etiqueta
Sin Etiquetas, Sea el primero en etiquetar este registro!
|
id |
oai:doaj.org-article:85d1410562734444aea958f3485cbe53 |
---|---|
record_format |
dspace |
spelling |
oai:doaj.org-article:85d1410562734444aea958f3485cbe532021-12-02T00:07:19ZEnhanced oral bioavailability of valsartan using a polymer-based supersaturable self-microemulsifying drug delivery system1178-2013https://doaj.org/article/85d1410562734444aea958f3485cbe532017-05-01T00:00:00Zhttps://www.dovepress.com/enhanced-oral-bioavailability-of-valsartan-using-a-polymer-based-super-peer-reviewed-article-IJNhttps://doaj.org/toc/1178-2013Dong Woo Yeom,1,* Bo Ram Chae,2,* Ho Yong Son,1 Jin Han Kim,1 Jun Soo Chae,1 Seh Hyon Song,2 Dongho Oh,2 Young Wook Choi1 1College of Pharmacy, Chung-Ang University, Seoul, 2Daewon Pharm. Co., Ltd, Seoul, Republic of Korea *These authors contributed equally to this work Abstract: A novel, supersaturable self-microemulsifying drug delivery system (S-SMEDDS) was successfully formulated to enhance the dissolution and oral absorption of valsartan (VST), a poorly water-soluble drug, while reducing the total quantity for administration. Poloxamer 407 is a selectable, supersaturating agent for VST-containing SMEDDS composed of 10% Capmul® MCM, 45% Tween® 20, and 45% Transcutol® P. The amounts of SMEDDS and Poloxamer 407 were chosen as formulation variables for a 3-level factorial design. Further optimization was established by weighting different levels of importance on response variables for dissolution and total quantity, resulting in an optimal S-SMEDDS in large quantity (S-SMEDDS_LQ; 352 mg in total) and S-SMEDDS in reduced quantity (S-SMEDDS_RQ; 144.6 mg in total). Good agreement was observed between predicted and experimental values for response variables. Consequently, compared with VST powder or suspension and SMEDDS, both S-SMEDDS_LQ and S-SMEDDS_RQ showed excellent in vitro dissolution and in vivo oral bioavailability in rats. The magnitude of dissolution and absorption-enhancing capacities using quantity-based comparisons was in the order S-SMEDDS_RQ > S-SMEDDS_LQ > SMEDDS > VST powder or suspension. Thus, we concluded that, in terms of developing an effective SMEDDS preparation with minimal total quantity, S-SMEDDS_RQ is a promising candidate. Keywords: valsartan, SMEDDS, supersaturation, factorial design, optimization, bio­availability Yeom DWChae BRSon HYKim JHChae JSSong SHOh DChoi YWDove Medical PressarticleValsartanSMEDDSSupersaturationFactorial designOptimizationBioavailabilityMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol Volume 12, Pp 3533-3545 (2017) |
institution |
DOAJ |
collection |
DOAJ |
language |
EN |
topic |
Valsartan SMEDDS Supersaturation Factorial design Optimization Bioavailability Medicine (General) R5-920 |
spellingShingle |
Valsartan SMEDDS Supersaturation Factorial design Optimization Bioavailability Medicine (General) R5-920 Yeom DW Chae BR Son HY Kim JH Chae JS Song SH Oh D Choi YW Enhanced oral bioavailability of valsartan using a polymer-based supersaturable self-microemulsifying drug delivery system |
description |
Dong Woo Yeom,1,* Bo Ram Chae,2,* Ho Yong Son,1 Jin Han Kim,1 Jun Soo Chae,1 Seh Hyon Song,2 Dongho Oh,2 Young Wook Choi1 1College of Pharmacy, Chung-Ang University, Seoul, 2Daewon Pharm. Co., Ltd, Seoul, Republic of Korea *These authors contributed equally to this work Abstract: A novel, supersaturable self-microemulsifying drug delivery system (S-SMEDDS) was successfully formulated to enhance the dissolution and oral absorption of valsartan (VST), a poorly water-soluble drug, while reducing the total quantity for administration. Poloxamer 407 is a selectable, supersaturating agent for VST-containing SMEDDS composed of 10% Capmul® MCM, 45% Tween® 20, and 45% Transcutol® P. The amounts of SMEDDS and Poloxamer 407 were chosen as formulation variables for a 3-level factorial design. Further optimization was established by weighting different levels of importance on response variables for dissolution and total quantity, resulting in an optimal S-SMEDDS in large quantity (S-SMEDDS_LQ; 352 mg in total) and S-SMEDDS in reduced quantity (S-SMEDDS_RQ; 144.6 mg in total). Good agreement was observed between predicted and experimental values for response variables. Consequently, compared with VST powder or suspension and SMEDDS, both S-SMEDDS_LQ and S-SMEDDS_RQ showed excellent in vitro dissolution and in vivo oral bioavailability in rats. The magnitude of dissolution and absorption-enhancing capacities using quantity-based comparisons was in the order S-SMEDDS_RQ > S-SMEDDS_LQ > SMEDDS > VST powder or suspension. Thus, we concluded that, in terms of developing an effective SMEDDS preparation with minimal total quantity, S-SMEDDS_RQ is a promising candidate. Keywords: valsartan, SMEDDS, supersaturation, factorial design, optimization, bio­availability |
format |
article |
author |
Yeom DW Chae BR Son HY Kim JH Chae JS Song SH Oh D Choi YW |
author_facet |
Yeom DW Chae BR Son HY Kim JH Chae JS Song SH Oh D Choi YW |
author_sort |
Yeom DW |
title |
Enhanced oral bioavailability of valsartan using a polymer-based supersaturable self-microemulsifying drug delivery system |
title_short |
Enhanced oral bioavailability of valsartan using a polymer-based supersaturable self-microemulsifying drug delivery system |
title_full |
Enhanced oral bioavailability of valsartan using a polymer-based supersaturable self-microemulsifying drug delivery system |
title_fullStr |
Enhanced oral bioavailability of valsartan using a polymer-based supersaturable self-microemulsifying drug delivery system |
title_full_unstemmed |
Enhanced oral bioavailability of valsartan using a polymer-based supersaturable self-microemulsifying drug delivery system |
title_sort |
enhanced oral bioavailability of valsartan using a polymer-based supersaturable self-microemulsifying drug delivery system |
publisher |
Dove Medical Press |
publishDate |
2017 |
url |
https://doaj.org/article/85d1410562734444aea958f3485cbe53 |
work_keys_str_mv |
AT yeomdw enhancedoralbioavailabilityofvalsartanusingapolymerbasedsupersaturableselfmicroemulsifyingdrugdeliverysystem AT chaebr enhancedoralbioavailabilityofvalsartanusingapolymerbasedsupersaturableselfmicroemulsifyingdrugdeliverysystem AT sonhy enhancedoralbioavailabilityofvalsartanusingapolymerbasedsupersaturableselfmicroemulsifyingdrugdeliverysystem AT kimjh enhancedoralbioavailabilityofvalsartanusingapolymerbasedsupersaturableselfmicroemulsifyingdrugdeliverysystem AT chaejs enhancedoralbioavailabilityofvalsartanusingapolymerbasedsupersaturableselfmicroemulsifyingdrugdeliverysystem AT songsh enhancedoralbioavailabilityofvalsartanusingapolymerbasedsupersaturableselfmicroemulsifyingdrugdeliverysystem AT ohd enhancedoralbioavailabilityofvalsartanusingapolymerbasedsupersaturableselfmicroemulsifyingdrugdeliverysystem AT choiyw enhancedoralbioavailabilityofvalsartanusingapolymerbasedsupersaturableselfmicroemulsifyingdrugdeliverysystem |
_version_ |
1718403938500214784 |