Formulation and in vivo assessment of baicalein solid lipid nanoparticles for enhanced brain delivery

摘要

The solid lipid nanoparticles (SLN) of baicalein prepared with Gelucire (62/5, 48/9, 44/14) or glyceryl monostearate as lipid phase and vitamin C and vitamin E as antioxidant to increase the stability of formulations. The SLN formulation was evaluated by measuring the particle size distribution and the stability of baicalein during the six-day storage. The highest entrapment efficiency of SLN was composed of Gelucire 62/5 with 8 mg of Vitamin C, and then was administrated into the rat by intravenous injection. The pharmacokinetics and biodistribution of baicalein in plasma and brain tissue were evaluated in vivo. It was found that baicalein formulated by SLN could extend the t_(1/2) and MRT about 1 hr, decrease the clearance and increase the AUC in plasma. The peak concentration (C_(max))of baicalein-SLN was 5-fold higher than that resulted from baicalein-solution and thereby increased the plasma concentration. It was suggested that SLN could extend the period of baicalein in blood and high concentration of baicalein was found in brain of the rat. Therefore, it proved that baicalein could transport through the blood-brain barrier by SLN with Gelucire 62/5.