PLoS ONE · 2014 · 43 citations · 33 references
These results show that membrane interactions play a prominent role during intestinal translocation of an acylated peptide. Acylation benefits permeation for shorter and medium chains due to increased membrane interactions, however, for longer chains insertion in the membrane becomes dominant and hinders translocation, i.e. the peptides get 'stuck' in the cell membrane. Applying a transcellular absorption enhancer increases the dynamics of membrane insertion and detachment by fluidizing the membrane, thus facilitating its effects primarily on membrane associated peptides.
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Lotte Bjerre Knudsen, Per F. Nielsen, Per Olaf Huusfeldt et al. · Journal of Medicinal Chemistry · 2000 · 681 citations · Full text
Peptide Engineering, Glycobiology, Once Daily Administration +21