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Controlling the gastrointestinal fate of nutraceutical‐enriched lipid nanoparticles: From mixed micelles to chylomicrons
Author(s) -
Yao Mingfei,
McClements David,
Zhao Faqing,
Craig Roger,
Xiao Hang
Publication year - 2015
Publication title -
the faseb journal
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.709
H-Index - 277
eISSN - 1530-6860
pISSN - 0892-6638
DOI - 10.1096/fasebj.29.1_supplement.249.6
Subject(s) - chylomicron , nutraceutical , micelle , solid lipid nanoparticle , chemistry , nanoparticle , food science , nanotechnology , biochemistry , materials science , organic chemistry , lipoprotein , cholesterol , very low density lipoprotein , aqueous solution
The oral bioavailability of lipophilic nutraceuticals can be greatly enhanced by lipid nanoparticle‐based delivery systems. These lipid nanoparticles are dissembled in the gastrointestinal tract to form mixed micelles that are then reassembled into chylomicrons within enterocytes and secreted into the lymph. In this study, we examined the influence of fatty acid type on the properties of mixed micelles and chylomicrons, and on the uptake of a highly lipophilic nutraceutical 5‐demethylnobiletin (5‐DN, found in citrus fruits). There were distinct differences in the structural properties of chylomicrons formed depending on fatty acid unsaturation. Oleic acid (C 18:1 ) was most effective at enhancing transport of 5‐DN and led to the formation of the largest chylomicrons. Linoleic acid (C 18:2 ) and linolenic acid (C 18:3 ) also promoted 5‐DN incorporation into chylomicrons, but they were less efficient than oleic acid. The metabolism of 5‐DN within the epithelium cells was greatly reduced when they were incorporated into chylomicrons, presumably because they were isolated from metabolic enzymes in the cytoplasm. These results have important implications for the design of lipid nanoparticle‐based delivery systems for lipophilic nutraceuticals by targeting them to the lymphatic circulation.