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

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 an...

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Main Authors: Wang Fengling, Chen Jin, Dai Wenting, He Zhengmin, Zhai Dandan, Chen Weidong
Format: Article
Language:English
Published: Sciendo 2017-09-01
Series:Acta Pharmaceutica
Subjects:
Online Access:https://doi.org/10.1515/acph-2017-0021
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spelling doaj-7768acb8d18f4bd6861124451df0f9432021-09-06T19:39:39ZengSciendoActa Pharmaceutica1846-95582017-09-0167335737110.1515/acph-2017-0021acph-2017-0021Pharmacokinetic studies and anticancer activity of curcumin-loaded nanostructured lipid carriersWang Fengling0Chen Jin1Dai Wenting2He Zhengmin3Zhai Dandan4Chen Weidong5Department of Pharmacy, The Second People’s Hospital of Hefei, Hefei230011, Anhui, People’s Republic of ChinaDepartment of Pharmacy, The Second People’s Hospital of Hefei, Hefei230011, Anhui, People’s Republic of ChinaDepartment of Pharmacy, The Second People’s Hospital of Hefei, Hefei230011, Anhui, People’s Republic of ChinaDepartment of Pharmacy, The Second People’s Hospital of Hefei, Hefei230011, Anhui, People’s Republic of ChinaDepartment of Pharmacy, The Second People’s Hospital of Hefei, Hefei230011, Anhui, People’s Republic of ChinaInstitute of Pharmacokinetics, Anhui University of Chinese Medicine, Hefei230012, Anhui, People’s Republic of ChinaIn 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.https://doi.org/10.1515/acph-2017-0021curcuminnanostructured lipid carrierspharmacokineticanticancer effectslung adenocarcinoma
collection DOAJ
language English
format Article
sources DOAJ
author Wang Fengling
Chen Jin
Dai Wenting
He Zhengmin
Zhai Dandan
Chen Weidong
spellingShingle Wang Fengling
Chen Jin
Dai Wenting
He Zhengmin
Zhai Dandan
Chen Weidong
Pharmacokinetic studies and anticancer activity of curcumin-loaded nanostructured lipid carriers
Acta Pharmaceutica
curcumin
nanostructured lipid carriers
pharmacokinetic
anticancer effects
lung adenocarcinoma
author_facet Wang Fengling
Chen Jin
Dai Wenting
He Zhengmin
Zhai Dandan
Chen Weidong
author_sort Wang Fengling
title Pharmacokinetic studies and anticancer activity of curcumin-loaded nanostructured lipid carriers
title_short Pharmacokinetic studies and anticancer activity of curcumin-loaded nanostructured lipid carriers
title_full Pharmacokinetic studies and anticancer activity of curcumin-loaded nanostructured lipid carriers
title_fullStr Pharmacokinetic studies and anticancer activity of curcumin-loaded nanostructured lipid carriers
title_full_unstemmed Pharmacokinetic studies and anticancer activity of curcumin-loaded nanostructured lipid carriers
title_sort pharmacokinetic studies and anticancer activity of curcumin-loaded nanostructured lipid carriers
publisher Sciendo
series Acta Pharmaceutica
issn 1846-9558
publishDate 2017-09-01
description 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.
topic curcumin
nanostructured lipid carriers
pharmacokinetic
anticancer effects
lung adenocarcinoma
url https://doi.org/10.1515/acph-2017-0021
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