Control of oral absorption of nutritional supplement using lipid-based formulations (LBFs): Application to the poorly water-soluble ingredient

Journal of Drug Delivery Science and Technology(2020)

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摘要
Among various formulations for oral use, lipid-based formulation (LBF) has been expected as a promising technology to improve the absorption of poorly water-soluble compounds. In the current study, three types of LBFs were tested for their effects on the extent, rate and variability of oral absorption of sesamin. Olive oil (type 1), type 3A-MC (medium-chain lipids) and type 3A-LC (long-chain lipids) formulations were prepared to test the intestinal absorption of sesamin in rats. Both type 3A formulations showed a rapid absorption of sesamin with minimized inter-individual variability compared to Olive oil formulation. Extent of absorption was in the order of 3A-LC > Olive oil > 3A-MC ≫ powder suspension. It was revealed that 3A-LC formulation kept the high solubilization capacity even under the lipid-digestive condition giving a high concentration of free sesamin. In the dog study, 3A-LC formulation also showed a high and less-variable absorption of sesamin, although the absorption was subjected to the effect of food intake. In conclusion, the extent, rate and variability of oral absorption of sesamin could be controlled by using different types of LBFs, indicating the possibility to develop better oral products of supplements using appropriate formulations.
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关键词
Lipid-based formulation,Self-microemulsifying drug delivery system,Sesamin,Oral absorption
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