title: Nanostructured lipid carriers for parenteral delivery of silybin: Biodistribution and pharmacokinetic studies.
abstract: 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.
authors.affiliation: Department of Pharmaceutics, College of Pharmacy, Shandong University, 44 Wenhua Xilu, Jinan 250012, PR China.
authors.forename: Lejiao
authors.initials: L
authors.lastname: Jia
authors.forename: Dianrui
authors.initials: D
authors.lastname: Zhang
authors.forename: Zhenyu
authors.initials: Z
authors.lastname: Li
authors.forename: Cunxian
authors.initials: C
authors.lastname: Duan
authors.forename: Yancai
authors.initials: Y
authors.lastname: Wang
authors.forename: Feifei
authors.initials: F
authors.lastname: Feng
authors.forename: Feihu
authors.initials: F
authors.lastname: Wang
authors.forename: Yue
authors.initials: Y
authors.lastname: Liu
authors.forename: Qiang
authors.initials: Q
authors.lastname: Zhang
mesh_terms: 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*
chemical_list: D004337:Drug Carriers; D008055:Lipids; D012838:Silymarin; D000077385:Silybin