A novel solid dispersion system for natural product-loaded medicine: silymarin-loaded solid dispersion with enhanced oral bioavailability and hepatoprotective activity.
A surface-attached silymarin-loaded solid dispersion with improved dissolution profile and enhanced oral bioavailability was formulated using silymarin, polyvinylpyrrolidone (PVP) and Tween 80 in water. In this solid dispersion, hydrophilic PVP was adhered onto the surface of crystalline drug rendering silymarin hydrophilic without changing its crystallinity. The drug solubility from the optimised solid dispersion prepared with silymarin/PVP/Tween 80 at the weight ratio of 5/2.5/2.5 increased by almost 650-fold compared to drug powder. The drug was physically and chemically stable in the solid dispersion for at least 6 months. Moreover, the solid dispersion enhanced the oral bioavailability of the drug in rats by almost 3-fold compared to the commercial product. The silymarin-loaded solid dispersion also exhibited advanced hepatoprotective bioactivity against CCl4-induced liver damage compared to silymarin or the commercial product. Thus, this silymarin-loaded solid dispersion would be useful for the enhancement of oral bioavailability and hepatoprotective activity of poorly water-soluble silymarin.
College of Pharmacy, Yeungnam University , Gyongsan , South Korea and.
Du Hyeong
du H
Hwang
Yong-Il
YI
Kim
Kwan Hyung
KH
Cho
Bijay Kumar
BK
Poudel
Ju Yeon
JY
Choi
Dong-Wuk
DW
Kim
Young-Jun
YJ
Shin
Ok-Nam
ON
Bae
Abid Mehmood
AM
Yousaf
Chul Soon
CS
Yong
Jong Oh
JO
Kim
Han-Gon
HG
Choi
D000284:Administration, Oral; D000818:Animals; D000975:Antioxidants / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D001682:Biological Availability; D002252:Carbon Tetrachloride Poisoning / Q000188:drug therapy / Q000378:metabolism; D010592:Pharmaceutic Aids / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D011136:Polysorbates; D011205:Povidone / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D051381:Rats; D012838:Silymarin / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D013501:Surface-Active Agents / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology
D000975:Antioxidants; D010592:Pharmaceutic Aids; D011136:Polysorbates; D012838:Silymarin; D013501:Surface-Active Agents; D011205:Povidone
Bioavailability; hepatoprotection; silymarin; solid dispersion; solubility