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Pharmacokinetics of intramuscular microparticle depot of valdecoxib in an experimental model

Sagar M Agnihotri1, Pradeep R Vavia

  • 1Pharmaceutical Division, Institute of Chemical Technology, University of Mumbai, Matunga, Mumbai, India. agnihotrisagar@hotmail.com

Drug Development and Industrial Pharmacy
|April 15, 2009
PubMed
Abstract

Insights

Injectable Valdecoxib (VC) microparticles offer sustained drug levels for 49 days in rabbits. This approach enhances drug bioavailability, potentially improving rheumatoid arthritis management by reducing dosing frequency.

Area of Science:

  • Pharmacology
  • Biomaterials Science
  • Drug Delivery Systems

Background:

  • Rheumatoid arthritis (RA) management requires effective pain and inflammation control.
  • Current treatment regimens for RA may involve frequent dosing, impacting patient compliance.
  • Valdecoxib (VC) is a cyclooxygenase-2 selective inhibitor used for inflammation.

Purpose of the Study:

  • To investigate the pharmacokinetics of a single intramuscularly administered Valdecoxib (VC) polymeric microparticle formulation.
  • To evaluate the sustained release and bioavailability of VC from poly[lac(glc-leu)] microparticles.

Main Methods:

  • Polymeric microparticles encapsulating Valdecoxib (VC) were prepared using an emulsion and solvent evaporation technique.
  • The microparticles were administered intramuscularly to New Zealand white rabbits for pharmacokinetic analysis.
  • Plasma drug concentrations were monitored over time to determine pharmacokinetic parameters.

Main Results:

  • A single intramuscular dose of Valdecoxib (VC)-loaded poly[lac(glc-leu)] microparticles achieved sustained therapeutic drug levels in plasma for 49 days.
  • The relative bioavailability of VC from the microparticle formulation was significantly increased compared to the unencapsulated drug.
  • The formulation demonstrated a prolonged drug release profile.

Conclusions:

  • Injectable poly[lac(glc-leu)] microparticles demonstrate potential for enhancing drug bioavailability.
  • This formulation may reduce dosing frequency, offering a promising strategy for improved rheumatoid arthritis management.
  • Sustained release of Valdecoxib (VC) via microparticles could lead to better therapeutic outcomes.

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