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

• DOI: 10.2147/ijn.s50683
• Publication Date: 2013-08-27T20:19:43Z
• Authors: Han-Gon Choi; Chul Soon Yong; Kwan Yeol Yang; Du Hyeong Hwang; Dong-Wuk Kim; Ok-Nam Bae; Jong Oh Kim; Young-Jun Shin; Abid Mehmood Yousaf; Yong-Il Kim
• Keywords: Polyvinylpyrrolidone; Membrane emulsification

Background: The purpose of this study was to develop a novel silymarin-loaded solid nanoparticle system with enhanced oral bioavailability and an ability provide excellent hepatic protection for poorly water-soluble drugs using Shirasu porous glass (SPG) membrane emulsification spray-drying technique. Methods: A liquid nanoemulsion formulated by applying the SPG This further converted into state nanosized particles physicochemical characteristics these nanoparticles were determined scanning electron microscopy, differential calorimetry, powder X-ray diffraction. Their dissolution, bioavailability, hepatoprotective activity in rats assessed comparison commercially available product. Results: Formulation nanoemulsion, comprising silymarin, castor oil, polyvinylpyrrolidone, Transcutol HP, Tween 80, water at weight ratio 5/3/3/1.25/1.25/100 accomplished technique agitator speed 700 rpm, feed pressure 15 kPa, continuous phase temperature 25°C. resulted generation comparatively uniform emulsion globules narrow size distribution. Moreover, nanoparticles, containing silymarin/castor oil/polyvinylpyrrolidone/Transcutol HP/Tween 80 5/3/3/1.25/1.25, improved about 1,300-fold drug solubility retained mean 210 nm. Silymarin located unaltered crystalline form nanoparticles. dissolved rapidly from reaching nearly 80% within minutes, indicating three-fold better dissolution than that commercial Further, showed considerably shorter time peak concentration, greater area under concentration-time curve, higher maximum concentration silymarin compared product ( P < 0.05). In particular, curve provided approximately 1.3-fold addition, significantly reduced carbon tetrachloride-induced hepatotoxicity, bioactivity Conclusion: Silymarin-loaded developed techniques could be useful delivery while affording protection. Keywords: nanoparticle, activity, membrane,