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British Journal of Anaesthesia, Vol 75, Issue 3 319-325, Copyright © 1995 by The Board of Management and Trustees of the British Journal of Anaesthesia

LABORATORY INVESTIGATIONS

Biodistribution of liposome-associated bupivacaine after extradural administration to rabbits

J. G. Boogaerts, N. D. Lafont, S. Carlino, E. Noel, P. Raynal, G. Goffinet and F. J. Legros
Department of Anaesthesiology, City Hospital, 6000 Charleroi, Belgium; Department of Anaesthesiology, Flemish Free University of Brussels Medical Centre, 101 Laarbeeklaan, 1090 Brussels, Belgium; Laboratory of Clinical Biology, Ambroise Pare Hospital, Mons, Belgium; Department of Surgery, CHU Andre Vesale, Montignies-le-Tilleul, Belgium; Laboratory of General Biology and Ultrastructural Morphology, University of Liege, Liege, Belgium

After one extradural injection of 0.25% bupivacaine 0.3 ml and 3H- bupivacaine 0.005 mCi in multilamellar liposomes, no systemic radioactivity (plasma, liver, heart muscle) was obtained for 1 h, and the labelling was less than that of systemic distribution of plain bupivacaine for the following 3 h. In contrast, radioactivity in the lumbar spinal nerves peaked in the first hour and remained higher than that of plain bupivacaine for 4 h. No radioactivity was measured in cerebrospinal fluid. Small unilamellar vesicles incorporating 3H- cholesterol did not significantly label spinal nerves and central nervous structures indicating that the mode of action of liposomal bupivacaine did not involve uptake by nerve structures. Rapid uptake of radioactivity by spinal nerves suggested exchange of bupivacaine between liposomes and nerve sheaths.
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