Polysorbate 80 promoted chylomicron secretion in Caco-2 cells and counteracted the inhibitory effects of other surfactants. These properties, in tandem with its P-gp inhibitory activity, make polysorbate 80 an ideal excipient for lymphotrophic vehicles. The ability to predict the in vivo response to Polysorbate 80 implies that the Caco-2 model is useful for studying absorption mechanisms from oral lipid-based formulations.
The ability of such bioactive excipients to simultaneously manipulate different cellular processes must be considered in selecting excipients for oral drug delivery systems. Such information is particularly relevant when the drug is lipophilic, a candidate for P-glycoprotein efflux, and where intestinal lymphatic targeting via chylomicron stimulation is desirable.
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