Preparation and pharmacokinetic evaluation of Tashinone IIA solid lipid nanoparticles.
Tashinone IIA loaded solid lipid nanoparticles (TA-SLN) coated with poloxamer 188 was prepared by emulsification/evaporation. The TA-SLN was characterized by transmission electron microscope and dynamic light scattering (DLS). The results showed that the TA-SLN had an average diameter of 98.7 nm with a zeta potential of - 31.6 mv and the drug loading of 4.6% and entrapment efficiency of 87.7%. In vitro release experiment showed that the release of Tashinone IIA from TA-SLN was in accordance with the Weibull equation. The best model fitting experimental data was a two-compartment open model with first-order. The area under curve of plasma concentration-time (AUC) and mean residence time (MRT) of TA-SLN were much higher than those of Tashinone IIA control solution (TA-SOL). The results of pharmacokinetic studies in rabbits indicated that the formulation of TA-SLN was successful in providing a delivery of slow release of Tashinone IIA.
Liu
Jianping
J
Department of Pharmaceutics, China Pharmaceutical University, Nanjing, P.R. China. liujianpingljp@hotmail.com
Zhu
Jiabi
J
Du
Zhiyong
Z
Qin
Bin
B
D045784:Abietanes; D000818:Animals; D019540:Area Under Curve; D001682:Biological Availability; D002851:Chromatography, High Pressure Liquid; D003692:Delayed-Action Preparations / Q000737:chemistry / Q000493:pharmacokinetics; D004058:Diffusion; D004339:Drug Compounding / Q000379:methods*; D004353:Drug Evaluation, Preclinical / Q000379:methods; D006207:Half-Life; D007275:Injections, Intravenous; D008027:Light; D008055:Lipids / Q000737:chemistry*; D046529:Microscopy, Electron, Transmission / Q000379:methods; D049329:Nanostructures / Q000737:chemistry* / Q000648:ultrastructure; D010316:Particle Size; D010616:Phenanthrenes / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics*; D010936:Plant Extracts / Q000097:blood / Q000737:chemistry / Q000493:pharmacokinetics*; D011817:Rabbits; D027544:Salvia / Q000737:chemistry*; D012542:Scattering, Radiation
D045784:Abietanes; D003692:Delayed-Action Preparations; D008055:Lipids; D010616:Phenanthrenes; D010936:Plant Extracts; C021751:tanshinone