Preparation and pharmacokinetics of curcumin nanostructured lipid carriers in rats

Curcumin (Cur) loaded nanostructured lipid carriers(Cur-NLC) was prepared by melt-emulsification method.The physicochemical properties such as morphology,particles size,Zeta potential,entrapment efficiency and drug-loading capability were evaluated.Dialysis method was employed to investigate the release of Cur-NLC in vitro.In addition,the pharmacokinetics in rats receiving oral dosing of Cur-NLC and Cur-dispersion was investigated by HPLC method and analyzed by DAS2.0 pharmacokinetic software.The result showed that Cur-NLC was quasi-spherical shapes observed by TEM and the mean particle size,Zeta potential,entrapment efficiency drug-loading capability and were (187.5±4.67)nm,(-23.65±2.86)mV,(98.33±0.40)% and (4.59±0.19)%,respectively.The cumulative release of Cur-NLC in 36 h was lower than that of Cur-dispersion in HCl (pH 1) and PBS (pH 6.8) (19.2% vs 84.2% and 24.3% vs 90.2%) and the release characteristic of Cur-NLC and Cur-dispersion displayed a first-order process and Peppas process,respectively.After oral administration the AUC and c_max of Cur-NLC were 19.12-fold and 17.22-fold higher than those of Cur-dispersion (621.14±179.92)ng·h/mL vs (32.49±3.55)ng·h/mL and (92.81±38.52)ng/mL vs (5.39±0.13) ng/mL.In conclusion,Cur-NLC exhibited high encapsulation efficiency and drug loading capability,possessed sustained release in vitro and improved the oral absorption and bioavailability of Cur when compared with Cur-dispersion.