Frank Jan, Schiborr Christina, Kocher Alexa, Meins Jürgen, Behnam Dariush, Schubert-Zsilavecz Manfred, Abdel-Tawab Mona
Institute of Biological Chemistry and Nutrition, University of Hohenheim, D-70599, Stuttgart, Germany.
Central Laboratory of German Pharmacists, Carl-Mannich-Str. 20, D-65760, Eschborn, Germany.
Plant Foods Hum Nutr. 2017 Mar;72(1):48-53. doi: 10.1007/s11130-016-0587-9.
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 cm, respectively). This resulted in a higher P value of 2.11 × 10 cm/s for Sol-CUR compared to a P value of 0.56 × 10 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.
姜黄素是姜科植物姜黄的活性成分，因其具有抗癌、抗炎、抗糖尿病和抗风湿特性，且在高达12克的非常高剂量下仍具有良好的耐受性和安全性，而越来越受到关注。基于吐温80的纳米胶束制剂是克服其低口服生物利用度的一种有前景的策略。因此，我们旨在研究在Caco-2细胞模型中天然姜黄素（CUR）与纳米胶束制剂（Sol-CUR）的摄取和跨上皮转运情况。Sol-CUR的通量高于CUR（分别为39.23与4.98μg·min·cm）。这导致Sol-CUR的P值为2.11×10 cm/s，高于CUR的P值0.56×10 cm/s。相应地，在180分钟的转运实验结束时，与CUR相比，Sol-CUR在基底外侧检测到的姜黄素量高出近9.5倍。姜黄素渗透率提高3.8倍，这与口服纳米胶束制剂后人类体内姜黄素的AUC相比天然姜黄素增加高达185倍的情况一致。本研究表明，胶束姜黄素制剂口服生物利用度的提高可能是小肠上皮细胞吸收增强和转运增加的结果。
