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 cmax 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.