Pharmacokinetics and Tissue Distribution of Oxymatrine-SLN

OBJECTIVE To study the pharmacokinetics and tissue distribution of oxymatrine-SLN in animal and investigate the liver targeting effect of oxymatrine-SLN. METHODS Oxymatrine-SLN composed of oxymatrine, phospholipid and stearic acid were prepared by “emulsion- evaporation- solidified at low temperature” process. The average diameter of the particles was 104 nm, Zeta potential was -32.6 mV, and encapsulation efficiency was 81.0%. The pharmacokinetics of rats after intravenous administration of oxymatrine-SLN and oxymatrine solution 100 mg·kg-1 was studied and the concentrations of oxymatrine in plasma, liver, lung, heart, spleen and kidney of mice were determined after intravenous administration 100 mg·kg-1 in mice.RESULTS The plasma concentration-time curves were discribed by a two-compartment model. The t1/2β of oxymatrine-SLN group was 5.5 times longer than oxymatrine solution group and the AUC of oxymatrine-SLN group was increased by 3.9 times compared with oxymatrine solution group. The tissue distribution of oxymatrine-SLN was different from that of free oxymatrine. The mean content of oxymatrine in liver at 30 min of oxymatrine-SLN group was 12 times greater than that of the oxymatrine solution group. Compared with oxymatrine solution, the relatively target efficiency to liver tissue was 360%.CONCLUSION It is demonstrated that oxymatrine-SLN has selective targeting to liver tissue and the liver targeted oxymatrine-SLN seem to have significant advantages and good development value.