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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 DW, Shin YJ, Bae ON, Kim YI, Kim JO, Yong CS, Choi HG

Received 28 June 2013

Accepted for publication 1 August 2013

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

DOI https://doi.org/10.2147/IJN.S50683

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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