Silymarin-loaded solid nanoparticles provide excellent hepatic protection: physicochemical characterization and in vivo evaluation

Kwan Yeol Yang,1,* Du Hyeong Hwang,1,* Abid Mehmood Yousaf,2 Dong Wuk Kim,2 Young-Jun Shin,2 Ok-Nam Bae,2 Yong-II Kim,1 Jong Oh Kim,1 Chul Soon Yong,1 Han-Gon Choi2 1College of Pharmacy, Yeungnam University, Dae-Dong, Gyongsan, 2College of Pharmacy and Institute of Pharmaceutical Science and Technol...

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Autores principales:	Yang KY, Hwang DH, Yousaf AM, Kim DW, Shin YJ, Bae ON, Kim YI, Kim JO, Yong CS, Choi HG
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2013
Materias:	Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/980eb21174eb481cad3eb354a080f419
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spelling	oai:doaj.org-article:980eb21174eb481cad3eb354a080f4192021-12-02T00:22:04ZSilymarin-loaded solid nanoparticles provide excellent hepatic protection: physicochemical characterization and in vivo evaluation1176-91141178-2013https://doaj.org/article/980eb21174eb481cad3eb354a080f4192013-08-01T00:00:00Zhttp://www.dovepress.com/silymarin-loaded-solid-nanoparticles-provide-excellent-hepatic-protect-a14180https://doaj.org/toc/1176-9114https://doaj.org/toc/1178-2013Kwan Yeol Yang,1,* Du Hyeong Hwang,1,* Abid Mehmood Yousaf,2 Dong Wuk Kim,2 Young-Jun Shin,2 Ok-Nam Bae,2 Yong-II Kim,1 Jong Oh Kim,1 Chul Soon Yong,1 Han-Gon Choi2 1College of Pharmacy, Yeungnam University, Dae-Dong, Gyongsan, 2College of Pharmacy and Institute of Pharmaceutical Science and Technology, Hanyang University, Sangnok-gu, Ansan, South Korea *These authors contributed equally to this work Background: The purpose of this study was to develop a novel silymarin-loaded solid nanoparticle system with enhanced oral bioavailability and an ability to provide excellent hepatic protection for poorly water-soluble drugs using Shirasu porous glass (SPG) membrane emulsification and a spray-drying technique. Methods: A silymarin-loaded liquid nanoemulsion was formulated by applying the SPG membrane emulsification technique. This was further converted into solid state nanosized particles by the spray-drying technique. The physicochemical characteristics of these nanoparticles were determined by scanning electron microscopy, differential scanning calorimetry, and powder X-ray diffraction. Their dissolution, bioavailability, and hepatoprotective activity in rats were assessed by comparison with a commercially available silymarin-loaded product. Results: Formulation of a silymarin-loaded nanoemulsion, comprising silymarin, castor oil, polyvinylpyrrolidone, Transcutol HP, Tween 80, and water at a weight ratio of 5/3/3/1.25/1.25/100 was accomplished using an SPG membrane emulsification technique at an agitator speed of 700 rpm, a feed pressure of 15 kPa, and a continuous phase temperature of 25°C. This resulted in generation of comparatively uniform emulsion globules with a narrow size distribution. Moreover, the silymarin-loaded solid nanoparticles, containing silymarin/castor oil/polyvinylpyrrolidone/Transcutol HP/Tween 80 at a weight ratio of 5/3/3/1.25/1.25, improved about 1,300-fold drug solubility and retained a mean size of about 210 nm. Silymarin was located in unaltered crystalline form in the nanoparticles. The drug dissolved rapidly from the nanoparticles, reaching nearly 80% within 15 minutes, indicating three-fold better dissolution than that of the commercial product. Further, the nanoparticles showed a considerably shorter time to peak concentration, a greater area under the concentration-time curve, and a higher maximum concentration of silymarin compared with the commercial product (P < 0.05). In particular, the area under the concentration-time curve of the drug provided by the nanoparticles was approximately 1.3-fold greater than that of the commercial product. In addition, the silymarin-loaded nanoparticles significantly reduced carbon tetrachloride-induced hepatotoxicity, indicating improved bioactivity compared with silymarin powder and the commercial product. Conclusion: Silymarin-loaded nanoparticles developed using SPG membrane emulsification and spray-drying techniques could be a useful system for delivery of poorly water-soluble silymarin while affording excellent hepatic protection. Keywords: silymarin, nanoparticle, hepatoprotective activity, Shirasu porous glass membrane, enhanced oral bioavailabilityYang KYHwang DHYousaf AMKim DWShin YJBae ONKim YIKim JOYong CSChoi HGDove Medical PressarticleMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol 2013, Iss default, Pp 3333-3343 (2013)
institution	DOAJ
collection	DOAJ
language	EN
topic	Medicine (General) R5-920
spellingShingle	Medicine (General) R5-920 Yang KY Hwang DH Yousaf AM Kim DW Shin YJ Bae ON Kim YI Kim JO Yong CS Choi HG Silymarin-loaded solid nanoparticles provide excellent hepatic protection: physicochemical characterization and in vivo evaluation
description	Kwan Yeol Yang,1,* Du Hyeong Hwang,1,* Abid Mehmood Yousaf,2 Dong Wuk Kim,2 Young-Jun Shin,2 Ok-Nam Bae,2 Yong-II Kim,1 Jong Oh Kim,1 Chul Soon Yong,1 Han-Gon Choi2 1College of Pharmacy, Yeungnam University, Dae-Dong, Gyongsan, 2College of Pharmacy and Institute of Pharmaceutical Science and Technology, Hanyang University, Sangnok-gu, Ansan, South Korea *These authors contributed equally to this work Background: The purpose of this study was to develop a novel silymarin-loaded solid nanoparticle system with enhanced oral bioavailability and an ability to provide excellent hepatic protection for poorly water-soluble drugs using Shirasu porous glass (SPG) membrane emulsification and a spray-drying technique. Methods: A silymarin-loaded liquid nanoemulsion was formulated by applying the SPG membrane emulsification technique. This was further converted into solid state nanosized particles by the spray-drying technique. The physicochemical characteristics of these nanoparticles were determined by scanning electron microscopy, differential scanning calorimetry, and powder X-ray diffraction. Their dissolution, bioavailability, and hepatoprotective activity in rats were assessed by comparison with a commercially available silymarin-loaded product. Results: Formulation of a silymarin-loaded nanoemulsion, comprising silymarin, castor oil, polyvinylpyrrolidone, Transcutol HP, Tween 80, and water at a weight ratio of 5/3/3/1.25/1.25/100 was accomplished using an SPG membrane emulsification technique at an agitator speed of 700 rpm, a feed pressure of 15 kPa, and a continuous phase temperature of 25°C. This resulted in generation of comparatively uniform emulsion globules with a narrow size distribution. Moreover, the silymarin-loaded solid nanoparticles, containing silymarin/castor oil/polyvinylpyrrolidone/Transcutol HP/Tween 80 at a weight ratio of 5/3/3/1.25/1.25, improved about 1,300-fold drug solubility and retained a mean size of about 210 nm. Silymarin was located in unaltered crystalline form in the nanoparticles. The drug dissolved rapidly from the nanoparticles, reaching nearly 80% within 15 minutes, indicating three-fold better dissolution than that of the commercial product. Further, the nanoparticles showed a considerably shorter time to peak concentration, a greater area under the concentration-time curve, and a higher maximum concentration of silymarin compared with the commercial product (P < 0.05). In particular, the area under the concentration-time curve of the drug provided by the nanoparticles was approximately 1.3-fold greater than that of the commercial product. In addition, the silymarin-loaded nanoparticles significantly reduced carbon tetrachloride-induced hepatotoxicity, indicating improved bioactivity compared with silymarin powder and the commercial product. Conclusion: Silymarin-loaded nanoparticles developed using SPG membrane emulsification and spray-drying techniques could be a useful system for delivery of poorly water-soluble silymarin while affording excellent hepatic protection. Keywords: silymarin, nanoparticle, hepatoprotective activity, Shirasu porous glass membrane, enhanced oral bioavailability
format	article
author	Yang KY Hwang DH Yousaf AM Kim DW Shin YJ Bae ON Kim YI Kim JO Yong CS Choi HG
author_facet	Yang KY Hwang DH Yousaf AM Kim DW Shin YJ Bae ON Kim YI Kim JO Yong CS Choi HG
author_sort	Yang KY
title	Silymarin-loaded solid nanoparticles provide excellent hepatic protection: physicochemical characterization and in vivo evaluation
title_short	Silymarin-loaded solid nanoparticles provide excellent hepatic protection: physicochemical characterization and in vivo evaluation
title_full	Silymarin-loaded solid nanoparticles provide excellent hepatic protection: physicochemical characterization and in vivo evaluation
title_fullStr	Silymarin-loaded solid nanoparticles provide excellent hepatic protection: physicochemical characterization and in vivo evaluation
title_full_unstemmed	Silymarin-loaded solid nanoparticles provide excellent hepatic protection: physicochemical characterization and in vivo evaluation
title_sort	silymarin-loaded solid nanoparticles provide excellent hepatic protection: physicochemical characterization and in vivo evaluation
publisher	Dove Medical Press
publishDate	2013
url	https://doaj.org/article/980eb21174eb481cad3eb354a080f419
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Silymarin-loaded solid nanoparticles provide excellent hepatic protection: physicochemical characterization and in vivo evaluation

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