Nanostructured lipid carriers for parenteral delivery of silybin: Biodistribution and pharmacokinetic studies.
The objective of the present study was to explore the potential of nanostructured lipid carriers (NLCs) for the intravenous delivery of silybin, a poorly water-soluble antihepatopathy agent. Silybin-NLC was prepared by the method of emulsion evaporation at a high temperature and solidification at a low temperature. The resultant NLC had a mean size 232.1 nm and a zeta potential of -20.7 mV. The differential scanning calorimetry (DSC) analysis indicated that silybin was not in crystalline state in the NLC. In vitro data for release of the drug from silybin-NLC was fitted to a two-stage exponential kinetic model. The pharmacokinetics and tissue distribution of silybin-NLC were studied after intravenous administration using New Zealand rabbits and Kunming mice as experimental animals. A silybin control solution was studied parallelly. Silybin-NLC showed higher AUC (area under tissue concentration-time curve) values and circulated in the blood stream for a longer time compared with silybin solution. The tissue distribution demonstrated a high uptake of silybin-NLC in RES organs particularly in liver. These results indicate that NLC is a potential sustained release and targeting system for silybin.
Jia
Lejiao
L
Department of Pharmaceutics, College of Pharmacy, Shandong University, 44 Wenhua Xilu, Jinan 250012, PR China.
Zhang
Dianrui
D
Li
Zhenyu
Z
Duan
Cunxian
C
Wang
Yancai
Y
Feng
Feifei
F
Wang
Feihu
F
Liu
Yue
Y
Zhang
Qiang
Q
D000818:Animals; D004337:Drug Carriers / Q000737:chemistry*; D008055:Lipids / Q000737:chemistry*; D051379:Mice; D046529:Microscopy, Electron, Transmission; D049329:Nanostructures / Q000737:chemistry*; D010316:Particle Size; D011817:Rabbits; D000077385:Silybin; D012838:Silymarin / Q000008:administration & dosage* / Q000493:pharmacokinetics*
D004337:Drug Carriers; D008055:Lipids; D012838:Silymarin; D000077385:Silybin