Acta Pharm. 67 (2017) 357-371

Original research paper

Pharmacokinetic studies and anticancer activity of curcumin-loaded nanostructured lipid carriers

FENGLING WANG, JIN CHEN, WENTING DAI, ZHENGMIN HE, DANDAN ZHAI and WEIDONG CHEN

¹ Department of Pharmacy, The Second People’s Hospital of Hefei, Hefei 230011, Anhui, People’s Republic of China

² Institute of Pharmacokinetics, Anhui University of Chinese Medicine, Hefei 230012, Anhui, People’s Republic of China

Accepted March 19, 2017

Published online May 16, 2017

In order to investigate the potential of nanostructured lipid carriers for efficient and targeted delivery of curcumin, the pharmacokinetic parameters of curcumin-loaded nanostructured lipid carriers (Cur-NLC) were evaluated in rats after a single intraperitoneal dose of Cur-NLC. In addition, the anticancer activity of Cur-NLC against human lung adenocarcinoma A549 cells was verified by a cellular uptake study, and a cytotoxicity and apoptosis assay. Bioavailability of Cur-NLC was better than that of native curcumin (p > 0.01), as seen from the area under the plasma concentration-time curve (AUC), maximum plasma concentration (C_max₎, mean residence time (MRT) and total plasma clearance (CL_z/F). Cur-NLC has a more obvious lung-targeting property in comparison with native curcumin. Cur-NLC showed higher anticancer activity in vitro against A549 cells than native curcumin (IC₅₀ value of 5.66 vs. 9.81 mg L^–1, respectively). Meanwhile, Cur-NLC treated A549 cells showed a higher apoptosis rate compared to that of native curcumin. These results indicate that NLC is a promising system for the delivery of curcumin in the treatment of lung adenocarcinoma.

Keywords: curcumin, nanostructured lipid carriers, pharmacokinetic, anticancer effects, lung adenocarcinoma