Biodistribution of liposome-associated bupivacaine after extradural administration to rabbits |
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Authors: | Boogaerts J G; Lafont N D; Carlino S; Noel E; Raynal P; Goffinet G; Legros F J |
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Institution: | 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 |
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Abstract: | 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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