TY  - JOUR
A1  - Frank, Jan
A1  - Schiborr, Christina
A1  - Kocher, Alexa
A1  - Meins, Jürgen
A1  - Behnam, Dariush
A1  - Schubert-Zsilavecz, Manfred
A1  - Abdel Tawab, Mona
T1  - Transepithelial transport of curcumin in caco-2 cells is significantly enhanced by micellar solubilisation
T2  - Plant foods for human nutrition
N2  - Curcumin, the active constituent of Curcuma longa L. (family Zingiberaceae), has gained increasing interest because of its anti-cancer, anti-inflammatory, anti-diabetic, and anti-rheumatic properties associated with good tolerability and safety up to very high doses of 12 g. Nanoscaled micellar formulations on the base of Tween 80 represent a promising strategy to overcome its low oral bioavailability. We therefore aimed to investigate the uptake and transepithelial transport of native curcumin (CUR) vs. a nanoscaled micellar formulation (Sol-CUR) in a Caco-2 cell model. Sol-CUR afforded a higher flux than CUR (39.23 vs. 4.98 μg min−1 cm−2, respectively). This resulted in a higher Papp value of 2.11 × 10−6 cm/s for Sol-CUR compared to a Papp value of 0.56 × 10−6 cm/s for CUR. Accordingly a nearly 9.5 fold higher amount of curcumin was detected on the basolateral side at the end of the transport experiments after 180 min with Sol-CUR compared to CUR. The determined 3.8-fold improvement in the permeability of curcumin is in agreement with an up to 185-fold increase in the AUC of curcumin observed in humans following the oral administration of the nanoscaled micellar formulation compared to native curcumin. The present study demonstrates that the enhanced oral bioavailability of micellar curcumin formulations is likely a result of enhanced absorption into and increased transport through small intestinal epithelial cells.
KW  - Absorption
KW  - Bioavailability
KW  - Caco-2 cells
KW  - Curcumin micelles
KW  - Transepithelial transport
KW  - Tween 80
Y1  - 2016
UR  - http://publikationen.ub.uni-frankfurt.de/frontdoor/index/index/docId/44119
UR  - https://nbn-resolving.org/urn:nbn:de:hebis:30:3-441193
SN  - 1573-9104
SN  - 0921-9668
N1  - Open Access: This article is distributed under the terms of the Creative Commons Attribution 4.0 International License (http:// creativecommons.org/licenses/by/4.0/), which permits unrestricted use, distribution, and reproduction in any medium, provided you give appropriate credit to the original author(s) and the source, provide a link to the Creative Commons license, and indicate if changes were made.
VL  - 72
IS  - 1
SP  - 48
EP  - 53
PB  - Springer Science + Business Media B.V ; Nijhoff
CY  - Dordrecht [u. a.]
ER  -