Preparation and In Vitro/In Vivo Evaluation of Microparticle Formulations Containing Meloxicam

Abstract

In this study, we have formulated chitosan-coated sodium alginate microparticles containing meloxicam (MLX) and aimed to investigate the correlation between in vitro release and in vivo absorbed percentages of meloxicam. The microparticle formulations were prepared by orifice ionic gelation method with two different sodium alginate concentrations, as 1% and 2% (w/v), in order to provide different release rates. Additionally, an oral solution containing 15 mg of meloxicam was administered as the reference solution for evaluation of in vitro/in vivo correlation (ivivc). Following in vitro characterization, plasma levels of MLX and pharmacokinetic parameters [elimination half-life (t (1/2)), maximum plasma concentration (C (max)), time for C (max) (t (max))] after oral administration to New Zealand rabbits were determined. Area under plasma concentration-time curve (AUC(0-a)) was calculated by using trapezoidal method. A linear regression was investigated between released% (in vitro) and absorbed% (in vivo) with a model-independent deconvolution approach. As a result, increase in sodium alginate content lengthened in vitro release time and in vivo t (max) value. In addition, for ivivc, linear regression equations with r (2) values of 0.8563 and 0.9402 were obtained for microparticles containing 1% and 2% (w/v) sodium alginate, respectively. Lower prediction error for 2% sodium alginate formulations (7.419 +/- 4.068) compared to 1% sodium alginate formulations (9.458 +/- 5.106) indicated a more precise ivivc for 2% sodium alginate formulation.