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Pig Journal Volume: 60
Publication date: December 2007

Research Papers

INTRA-CELLULAR ACCUMULATION AND TRANS-EPITHELIAL TRANSPORT OF AIVLOSIN, TYLOSIN AND TILMICOSIN
A.D. Stuart, T.D.K. Brown, G. Imrie, J.B. Tasker and A.P.A. Mockett

Abstract
The macrolide antibiotics aivlosin, tilmicosin and tylosin were tested for their ability to enter and accumulate inside a number of mammalian cell types including human gut epithelial cells, pig kidney epithelial cells and pig white blood cells. Aivlosin (3-acetyl-4 isovaleryltylosin) entered and was concentrated in all three cell types and was shown to rapidly (within 10 min.) concentrate in white blood cells. This antibiotic entered polarised human gut epithelial cells (Caco-2 cells) by either the apical or baso-lateral surface, to be concentrated inside the cells and to be transported to the opposite surface. Tylosin entered all cell types relatively poorly, whilst tilmicosin was intermediate in its ability to enter and accumulate in cells. The greater uptake of aivlosin may be related to the presence of an isovaleryl group. Although the three antibiotics are all macrolides, they were shown to differ in at least one aspect of distribution, relevant to their efficacy in treating clinical disease.

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