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

Authors Yang KY, Hwang DH, Yousaf AM, Kim D, Shin Y, Bae O, Kim Y, Kim JO, Yong CS, Choi H

Received 28 June 2013

Accepted for publication 1 August 2013

Published 28 August 2013 Volume 2013:8(1) Pages 3333—3343


Checked for plagiarism Yes

Review by Single-blind

Peer reviewer comments 3

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

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