Curcumin, a widely used spice in food has been associated with many health benefits, but its health-promoting potential is limited by its poor bioavailability. This is due to the fact that curcumin is poorly absorbed, and absorbed curcumin is subject to extensive biotransformation. However, the oral bioavailability of bioactive molecules could be greatly increased by engineered lipid nanoparticles (ELNs). After ingestion, these ELNs could be disassembled and reassembled into various types of biological lipid nanoparticales, <i>e.g.</i> mixed micelles and chylomicrons, as they pass through the gastrointestinal tract (GIT). Controlling the initial composition of ELNs could be used to alter the properties of mixed micelles and chylomicrons formed in GIT, in turn, influence the solubility, absorption and metabolism of nutraceuticals in GIT. In current project, we evaluated the influence of ELNs with different carrier oil types on the bioavailability of encapsulated curcumin. To better understand the bioavailability of curcumin, the metabolic fate of curcumin in the monolayer enterocyte model was established. Our results demonstrated that after being absorbed by the enterocytes from the apical side of the monolayer, curcumin underwent phase I metabolism to yield three metabolites. Curcumin and these phase I metabolites then were subject to phase II metabolism to yield their corresponding conjugated phase II metabolites in the enterocytes. Curcumin and these metabolites were then transported across enterocytes to the basolateral side of the monolayer. Curcumin was encapsulated in ELNs i.e. nanoemulsions made of different carrier oils (such as corn oil, olive oil, medium chain triglyceride (MCT) and long chain triglyceride (LCT)), and then subjected to simulated gastrointestinal digestion before it was exposed to the enterocyte monolayer. I was found that nanoemulsions profoundly influenced the absorption and metabolism of curcumin in the enterocytes. The olive oil-based nanoemulsion was more effective at enhancing trans-enterocyte transport of curcumin than nanoemulsions made of corn oil, MCT, and LCT. Moreover, the metabolism of curcumin was greatly reduced by nanoemulsions made of corn oil, olive oil, MCT, and LCT, which could have retained the bioactivities of curcumin. These results have important implications in the rational design of lipid nanoparticle-based delivery systems to enhance health benefits of nutraceuticals such as curcumin.

Absorption and metabolism of curcumin in different type of nanoemulsion

2019 Fall National Meeting

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