Objective: This study reports a preclinical evaluation of an alginate/chitosan nanoparticle formulation containing NovaBupi®, a racemic bupivacaine (BVC) containing 25% dextrobupivacaine and 75% levobupivacaine.
Methods: New Zealand White rabbits (n=6) received intraoral or intrathecal injections of BVC 0.5% or BVC 0.5%-loaded alginate-chitosan nanoparticles (BVC). BVC plasma levels and pharmacokinetic parameters were determined in blood samples of these rabbits. An infraorbital nerve blockade was performed in male Wistar rats (n=7) with the same formulations and the vehicle (NP). Histological evaluation of local toxicity after 6 hours and 24 hours of the treatments was performed in rats' (n=6) oral tissues.
Results: No statistically significant difference was observed between plasma concentrations and pharmacokinetic parameters (>0.05) after intraoral injections. However, after intrathecal injection BVC changed approximately three times the values of volume of distribution and area under the curve (AUC; <0.05). The total analgesic effect of BVC after infraorbital nerve blockade was improved by 1.4-fold (<0.001) with BVC. BVC and BVC did not induce significant local inflammatory reaction.
Conclusion: The encapsulation of BVC prolongs the local anesthetic effect after infraorbital nerve blockade and altered the pharmacokinetics after intrathecal injection.
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| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5896646 | PMC |
| http://dx.doi.org/10.2147/JPR.S158695 | DOI Listing |
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