Acta Pharmaceutica, Vol. 67 No. 3, 2017.
Original scientific paper
https://doi.org/10.1515/acph-2017-0022
Pharmacokinetic studies and anticancer activity of curcumin-loaded nanostructured lipid carriers
FENGLING WANG
orcid.org/0000-0002-7787-2638
; Department of Pharmacy, The Second People’s Hospital of Hefei, Hefei 230011, Anhui, People’s Republic of China; Institute of Pharmacokinetics, Anhui University of Chinese Medicine, Hefei 230012, Anhui, People’s Republic of China
JIN CHEN
orcid.org/0000-0002-6607-5705
; Department of Pharmacy, The Second People’s Hospital of Hefei, Hefei 230011, Anhui, People’s Republic of China
WENTING DAI
orcid.org/0000-0003-1884-6277
; Department of Pharmacy, The Second People’s Hospital of Hefei, Hefei 230011, Anhui, People’s Republic of China
ZHENGMIN HE
orcid.org/0000-0003-2846-7780
; Department of Pharmacy, The Second People’s Hospital of Hefei, Hefei 230011, Anhui, People’s Republic of China
DANDAN ZHAI
orcid.org/0000-0003-0865-2364
; Department of Pharmacy, The Second People’s Hospital of Hefei, Hefei 230011, Anhui, People’s Republic of China
WEIDONG CHEN
orcid.org/0000-0002-7787-2638
; Institute of Pharmacokinetics, Anhui University of Chinese Medicine, Hefei 230012, Anhui, People’s Republic of China
Abstract
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 (Cmax), mean residence time (MRT) and total plasma clearance (CLz/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
Hrčak ID:
181148
URI
Publication date:
30.9.2017.
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