کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
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5521502 | 1545306 | 2017 | 9 صفحه PDF | دانلود رایگان |
Curcumin (Cur) is a strong natural antioxidant, who can prevent multiple diseases such as anti-cancer, anti-inflammatory, have a resistance to alzheimer's disease and various malignant diseases. But it has poor oral bioavailability due to its poor aqueous solubility, as well as instability. While its novel derivatives (CB and FE), showed better anti-tumor activity, better anti-oxidant activity and better stability than the original drug (Cur). The aim of this study was to study the intestinal transport of Cur, CB and FE using an in vitro Caco-2 cell monolayer model. The results showed that Cur had a lower permeability coefficient (1.13 Ã 10â6 ± 0.11 Ã 10â6 cm/s) for apical-to-basolated (AP-BL) transport at 25 μM, while the transport rate for AP to BL flux of CB (3.18 Ã 10â6 ± 0.31 Ã 10â6 cm/s) and FE (5.28 Ã 10â6 ± 0.83 Ã 10â6 cm/s) were significantly greater than that of Cur. The efflux ratio (ER) value at the concentration of 25 μM was 1.31 for Cur, 1.26 for CB and 1.33 for FE, suggesting there was no active efflux involved in the translocation across the Caco-2 cell monolayers for the three compounds. Furthermore, the transport flux of CB and FE was in a concentration dependent manner, suggesting the intestinal transport mechanism in them was passive transport. In summary, the results demonstrated that both the intestinal permeability of CB and FE across Caco-2 cell monolayers was significantly improved compare to Cur. Thus they might show a higher oral bioavailability in vivo, and show the potential application in clinic or nutraceutical.
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Journal: European Journal of Pharmaceutics and Biopharmaceutics - Volume 117, August 2017, Pages 123-131