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Preparation and in vitro/in vivo evaluation of microparticle formulations containing meloxicam

Hakan Eroglu1, Nihan Burul-Bozkurt, Serdar Uma

  • 1Department of Pharmaceutical Technology, Faculty of Pharmacy, Hacettepe University, Sihhiye, Ankara, Turkey. ehakan@hacettepe.edu.tr

AAPS Pharmscitech
|November 22, 2011
PubMed

Insights

Chitosan-coated sodium alginate microparticles containing meloxicam were developed. Higher alginate concentrations improved the in vitro/in vivo correlation for meloxicam release, enhancing predictability.

Area of Science:

  • Pharmaceutical Sciences
  • Drug Delivery Systems
  • Pharmacokinetics

Background:

  • Chitosan-coated sodium alginate microparticles offer potential for controlled drug release.
  • Meloxicam (MLX) is a non-steroidal anti-inflammatory drug requiring optimized delivery systems.
  • Establishing in vitro-in vivo correlations (IVIVC) is crucial for predicting drug performance.

Purpose of the Study:

  • To formulate and characterize chitosan-coated sodium alginate microparticles containing meloxicam (MLX).
  • To investigate the correlation between in vitro drug release and in vivo absorption percentages of MLX.
  • To evaluate the impact of sodium alginate concentration on MLX release kinetics and IVIVC.

Main Methods:

  • Microparticles prepared using the orifice ionic gelation method with 1% and 2% sodium alginate.
  • In vitro release studies conducted to assess drug release profiles.
  • Pharmacokinetic studies in New Zealand rabbits to determine plasma MLX levels and parameters (Cmax, Tmax, t1/2).
  • Model-independent deconvolution and linear regression analysis used for IVIVC assessment.

Main Results:

  • Increased sodium alginate concentration (2% vs 1%) extended in vitro release time and in vivo Tmax.
  • High linearity (r² values of 0.8563 and 0.9402) observed between in vitro release and in vivo absorption for both formulations.
  • The 2% sodium alginate formulation demonstrated a more precise IVIVC with lower prediction error.

Conclusions:

  • Chitosan-coated sodium alginate microparticles are effective for MLX delivery.
  • Sodium alginate concentration significantly influences MLX release kinetics and IVIVC.
  • The 2% sodium alginate formulation provides a reliable predictor of in vivo performance, facilitating formulation optimization.

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