Effect of dose and dosage interval on the oral bioavailability of docetaxel in combination with a curcumin self-emulsifying drug delivery system (SEDDS)

Yan, Yi-Dong, Marasini, Nirmal, Choi, Young Keun, Kim, Jong Oh, Woo, Jong Soo, Yong, Chul Soon and Choi, Han Gon (2012) Effect of dose and dosage interval on the oral bioavailability of docetaxel in combination with a curcumin self-emulsifying drug delivery system (SEDDS). European Journal of Drug Metabolism and Pharmacokinetics, 37 3: 217-224. doi:10.1007/s13318-011-0078-1


Author Yan, Yi-Dong
Marasini, Nirmal
Choi, Young Keun
Kim, Jong Oh
Woo, Jong Soo
Yong, Chul Soon
Choi, Han Gon
Title Effect of dose and dosage interval on the oral bioavailability of docetaxel in combination with a curcumin self-emulsifying drug delivery system (SEDDS)
Journal name European Journal of Drug Metabolism and Pharmacokinetics   Check publisher's open access policy
ISSN 0378-7966
2107-0180
Publication date 2012-09
Year available 2011
Sub-type Article (original research)
DOI 10.1007/s13318-011-0078-1
Open Access Status Not Open Access
Volume 37
Issue 3
Start page 217
End page 224
Total pages 8
Place of publication Paris, France
Publisher Springer-Verlag France
Language eng
Formatted abstract
The present study investigated the effects of a curcumin self-emulsifying drug delivery systems (SEDDS) on the pharmacokinetics of orally administered docetaxel in rats. A single dose of docetaxel was orally administered (30 mg/kg) alone or after oral curcumin SEDDS (25, 50, 100 and 150 mg/kg) administration with time intervals of 0, 15 and 30 min, respectively. After oral administration, the Cmax and the area under the plasma concentration-time curve (AUC) of docetaxel were significantly increased (0 min, p<0.05; 15 and 30 min, p<0.01) by 2.2, 4.7 and 4.6 times and 2.0, 3.8 and 4.1 times compared to that of control group, respectively, after treatment with curcumin SEDDS (100 mg/kg) for each interval. Moreover, The Cmax of docetaxel was increased by 2.6 and 4.4 times in response to 25 and 50 mg/kg curcumin SEDDS treatment, respectively, the corresponding AUC was increased by about 2.4 and 3.1 times, and consequently the absolute bioavailabilities of docetaxel in these two treatment groups were 7.9 and 10.4%, respectively, which showed a significant increase of about 2.4- and 3.2-fold in comparison to the control value (3.3%). However, no further increase in either AUC or Cmax values of docetaxel was observed as the curcumin SEDDS dose was increased from 50 to 150 mg/kg. It is worth noting that the presence of curcumin SEDDS did not significantly decrease the systemic clearance, which was shown by the almost unchanged terminal half-life (t1/2) of docetaxel in all treatment groups. Thus, the enhanced bioavailability of oral docetaxel by curcumin SEDDS seemed to be likely due to an inhibition function of cytochrome P450 (CYP) 3A and P-glycoprotein (Pgp) in the intestines of the rats. However, further in vivo studies are needed to verify these hypotheses.
Keyword Bioavailability
Curcumin
Docetaxel
Pharmacokinetics
SEDDS
Q-Index Code C1
Q-Index Status Provisional Code
Institutional Status Non-UQ

Document type: Journal Article
Sub-type: Article (original research)
Collection: School of Chemistry and Molecular Biosciences
 
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