Sustained release of bupivacaine from devices based on chitosan.
Chitosan beads loaded with bupivacaine (16+/-3 microg of drug per milligram of beads) were prepared by cross-linking with glutaraldehyde. In vitro drug release at pH and temperature conditions similar to those of the biological systems were studied. Maximum release of bupivacaine was obtained between 100 and 120 h, depending on the presence of lysozyme in the release medium, since the enzyme facilitates the release process. A constant release rate of the drug, between 11 and 15 microg/h, was observed for 30 h. In order to prolong bupivacaine release, the drug-loaded chitosan beads were coated with a poly(DL-lactide-co-glycolide) film. The resulting device allows the drug to be released in a sustained form; a constant release rate between 28.5 and 29.5 microg/h was obtained for 3 days, and the maximum release of bupivacaine took place at day 9. The in vitro results indicate a possible application of these bupivacaine loaded chitosan systems as drug release devices with an analgesic action. Thus, they could be used in the treatment of dental pain in the buccal cavity, where drug release would be made easier by lysozyme of the saliva.
Bernardo
M V
MV
Departamento de Bioquímica y Biología Molecular, Facultad de Medicina, Universidad Complutense de Madrid, 28040 Madrid, Spain.
Blanco
M D
MD
Sastre
R L
RL
Teijón
C
C
Teijón
J M
JM
D002045:Bupivacaine / Q000737:chemistry / Q000493:pharmacokinetics*; D002686:Chitin / Q000031:analogs & derivatives* / Q000737:chemistry / Q000493:pharmacokinetics*; D048271:Chitosan; D003692:Delayed-Action Preparations / Q000737:chemistry / Q000493:pharmacokinetics
D003692:Delayed-Action Preparations; D002686:Chitin; D048271:Chitosan; D002045:Bupivacaine