Enhanced oral bioavailability of docetaxel in rats by four consecutive days of pre-treatment with curcumin
- Authors
- Yan, Yi-Dong; Kim, Dae Hwan; Sung, Jun Ho; Yong, Chul Soon; Choi, Han Gon
- Issue Date
- Oct-2010
- Publisher
- ELSEVIER
- Keywords
- Docetaxel; Curcumin; Pharmacokinetics; Bioavailability; Pre-treatment
- Citation
- INTERNATIONAL JOURNAL OF PHARMACEUTICS, v.399, no.1-2, pp.116 - 120
- Indexed
- SCIE
SCOPUS
- Journal Title
- INTERNATIONAL JOURNAL OF PHARMACEUTICS
- Volume
- 399
- Number
- 1-2
- Start Page
- 116
- End Page
- 120
- URI
- https://scholarworks.bwise.kr/erica/handle/2021.sw.erica/39447
- DOI
- 10.1016/j.ijpharm.2010.08.015
- ISSN
- 0378-5173
- Abstract
- As with many other anti-cancer agents, docetaxel is a substrate for ATP-binding cassette transporters such as P-glycoprotein and its metabolism is mainly catalysed by CYP3A. In order to improve the oral bioavailability of docetaxel, a component of turmeric, curcumin, which can down-regulate the intestinal P-glycoprotein and CYP3A protein levels, was used for the pre-treatment of rats before the oral administration of docetaxel. Curcumin (100 mg/kg) did not significantly modify the pharmacokinetics of docetaxel when given orally 30 min before the administration of docetaxel. However, the C-max of docetaxel in rats pre-treated with curcumin for four consecutive days was significantly increased (p < 0.01) by about 10 times compared to that of the docetaxel control, and the area under the plasma concentration-time curve (AUC) was about eight times higher than that of the control. Consequently, the absolute bioavailability of docetaxel in the treatment group (four days of curcumin at 100 mg/kg) was about 40%, which was a significant increase of about eightfold in comparison to the control value. Thus, the oral bioavailability of docetaxel was enhanced by the co-administration of regular curcumin. It could be possible to administer docetaxel orally, besides the established iv. route. Crown Copyright (C) 2010 Published by Elsevier B.V. All rights reserved.
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