Department of Food Science, Rutgers, the State University of New Jersey, 65 Dudley Road, New Brunswick, New Jersey 08901, United States.
J Agric Food Chem. 2011 Sep 14;59(17):9120-6. doi: 10.1021/jf201451m. Epub 2011 Aug 17.
Curcumin is a bioactive compound with poor oral bioavailability. Low water solubility and rapid metabolism are two known limiting factors, but the absorption mechanism of solubilized curcumin remains unclear. This study investigated the permeation mechanism of solubilized curcumin using an in vitro Caco-2 cell monolayer model. It was shown that curcumin permeated across the monolayers fairly rapidly [P(app)(A-B) = (7.1 ± 0.7) × 10(-6) cm/s] and the permeation mechanism was found as passive diffusion [P(app)(B-A)/P(app)(A-B) = 1.4]. Furthermore, the permeation rates of curcumin complexed with bovine serum albumin and in the bile salts-fatty acids mixed micelles were also determined as P(app)(mixed micelle) > P(app)(DMSO) > P(app)(protein complex). These results suggested that solubilization agents play an important role in the permeation of solubilized curcumin, and stronger binding between the solubilization agents and curcumin may decrease the permeation rate. The results further suggest that lipid-based formulations, which solubilize curcumin in mixed micelles after lipid digestion, are promising vehicles for curcumin oral delivery.
姜黄素是一种生物活性化合物，口服生物利用度差。低水溶性和快速代谢是两个已知的限制因素，但增溶姜黄素的吸收机制仍不清楚。本研究使用体外 Caco-2 细胞单层模型研究了增溶姜黄素的渗透机制。结果表明，姜黄素相当快速地穿过单层[P(app)(A-B)=(7.1±0.7)×10(-6)cm/s]，渗透机制为被动扩散[P(app)(B-A)/P(app)(A-B)=1.4]。此外，还测定了与牛血清白蛋白复合的姜黄素和胆汁盐-脂肪酸混合胶束中的姜黄素的渗透速率，结果为 P(app)(混合胶束)>P(app)(DMSO)>P(app)(蛋白复合物)。这些结果表明，增溶剂在增溶姜黄素的渗透中起着重要作用，增溶剂与姜黄素之间更强的结合可能会降低渗透速率。结果进一步表明，在脂质消化后将姜黄素增溶在混合胶束中的基于脂质的制剂是姜黄素口服递送的有前途的载体。
