Preparation of Curcumin-loaded Modifying Borneol Cationic Liposomes and Study on Its Brain Targeting Effect

OBJECTIVE To prepare curcumin-loaded modifying borneol cationic liposomes(Cur-BCLPs), and to investigate their pharmacokinetics in vivo and the brain tissue distribution after intranasal administration. METHODS Cur-BCLPs were prepared with ethanol injection method; the morphology of cationic liposomes was observed by transmission electron microscope; mean particle size was estimated by laser particle size analyzer; entrapment efficiency and drug loading were investigated by ultracentrifugation; using curcumin suspension(Cur-Sol) and borneol curcumin suspension(BO-Cur-Sol) as control group, the pharmacokinetic behavior in vivo and the concentration in brain of Cur-BCLPs after intranasal administration in rats were studied. The pharmacokinetic parameters were calculated by DAS 2.0. RESULTS The shape of cationic liposomes was roundness. The mean particle size was (105.99±2.40)nm, entrapment efficiency was (81.95±1.03)%, drug loading was (4.28±0.46)%, respectively. Results of pharmacokinetic study in vivo showed that the T_1/2 of Cur-Sol, BO-Cur-Sol and Cur-BCLPs were (4.27±1.53)h, (3.98±0.24)h and (6.01±0.63)h, AUC_0→t were (224.38±21.95)μg·h·L^-1, (243.40±12.26)μg·h·L^-1 and (562.28±24.30)μg·h·L^-1, clearance rate were (1.82±0.36)L·h^-1·kg^-1, (1.72±0.11)L·h^-1·kg^-1 and (0.78±0.03)L·h^-1·kg^-1,mean residence time were (4.28±0.23)h, (4.41±0.15)h and (8.09±0.17)h. Results of distribution in brain showed that AUC_0→tof Cur-Sol, BO-Cur-Sol and Cur-BCLPs were (29.82±1.10)μg·h·g^-1, (35.47±1.75)μg·h·g^-1 and(54.06±3.90)μg·h·g^-1, clearance rate were (15.73±0.84)L·h^-1·kg^-1, (13.23±0.52)L·h^-1·kg^-1and (8.52±0.92)L·h^-1·kg^-1. CONCLUSION Cur-BCLPs after intranasal administration may increase the concentration and slow their elimination in vivo and brain.