[Pharmacokinetics and pharmacodynamics of poly (lactide-co-glycolide) microspheres containing ropivacaine and dexamethasone for sciatic nerve block in mice]

Nan Fang Yi Ke Da Xue Xue Bao. 2010 Mar;30(3):502-5.
[Article in Chinese]

Abstract

Objective: To investigate the pharmacokinetics and pharmacodynamics of poly (lactide-co-glycolide) microspheres containing ropivacaine and dexamethasone for sciatic nerve block in mice.

Methods: A total of 165 female mice were randomly assigned into 3 groups, namely dexamethasone-loaded ropivacaine microsphere group (group A, n=55), ropivacaine microsphere group (group B, n=55) and PLGA microsphere group (group C, n=55). The mice received surgical implantation of the corresponding preparations near the sciatic nerve at the dose of 400 mg/kg. Hot plate test was used to evaluate the anesthetic effect of these microspheres at different time points after the implantation, and high-performance liquid chromatography (HPLC) was employed to determine plasma ropivacaine concentration.

Results: Pharmacodynamic study showed that the duration of sciatic nerve sensory block was significantly longer in group A than in group B (P<0.05). The analysis of pharmacokinetics variables demonstrated that T(1/2) in group A was prolonged as compared with that of group B. No anesthetic effect was observed in group C.

Conclusion: Dexamethasone-loaded ropivacaine microspheres can significantly prolong the analgesic effect of ropivacaine in mice.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amides / pharmacokinetics*
  • Amides / pharmacology
  • Anesthetics, Local / pharmacokinetics
  • Anesthetics, Local / pharmacology
  • Animals
  • Delayed-Action Preparations
  • Dexamethasone / pharmacokinetics*
  • Dexamethasone / pharmacology
  • Female
  • Lactic Acid / chemistry*
  • Mice
  • Microspheres
  • Nerve Block / methods*
  • Polyglycolic Acid / chemistry*
  • Polylactic Acid-Polyglycolic Acid Copolymer
  • Random Allocation
  • Ropivacaine
  • Sciatic Nerve*

Substances

  • Amides
  • Anesthetics, Local
  • Delayed-Action Preparations
  • Polylactic Acid-Polyglycolic Acid Copolymer
  • Polyglycolic Acid
  • Lactic Acid
  • Ropivacaine
  • Dexamethasone