Characterization of a Controlled Release Polymer-Meloxicam Matrix

Microstructure CQAs
Full field-of-view pharmaceutical tablet microstructure image showing internal phase distribution and pore network
Publication Title

Development of hot-melt extruded drug/polymer matrices for sustained delivery of meloxicam

For effective resolution of regional subacute inflammation and prevention of biofouling formation, we have developed a polymeric implant that can release meloxicam, a selective cyclooxygenase (COX)-2 inhibitor, in a sustained manner. Meloxicam-loaded polymer matrices were produced by hot-melt extrusion, with commercially available biocompatible polymers, poly(ε-caprolactone) (PCL), poly(lactide-co-glycolide) (PLGA), and poly(ethylene vinyl acetate) (EVA). PLGA and EVA had a limited control over the drug release rate partly due to the acidic microenvironment and hydrophobicity, respectively. PCL allowed for sustained release of meloxicam over two weeks and was used as a carrier of meloxicam. Solid-state and image analyses indicated that the PCL matrices encapsulated meloxicam in crystalline clusters, which dissolved in aqueous medium and generated pores for subsequent drug release. The subcutaneously implanted meloxicam-loaded PCL matrices in rats showed pharmacokinetic profiles consistent with their in vitro release kinetics, where higher drug loading led to faster drug release. This study finds that the choice of polymer platform is crucial to continuous release of meloxicam and the drug release rate can be controlled by the amount of drug loaded in the polymer matrices.

Publication cover: Characterization of controlled release polymer-meloxicam microsphere formulation

Yun-Chu Chen, Dana E. Moseson, Coralie A. Richard, Monica R. Swinney, Sarena D. Horava, Kaoutar Abbou Oucherif, Amy L. Cox, Eric D. Hawkins, Yongzhe Li, Daniel F. DeNeve, Joshua Lomeo, Aiden Zhu, L. Tiffany Lyle, Eric J. Munson, Lynne S. Taylor, Kinam Park, Yoon Yeo

Published with Eli Lilly and Purdue

https://doi.org/10.1016/j.jconrel.2021.12.038

AbbVie logo
AbbVie logo
Bausch Health logo
Bausch Health logo
Bristol Myers Squibb logo
Bristol Myers Squibb logo
Merck logo
Merck logo
Moderna logo
Moderna logo
Novartis logo
Novartis logo
Pfizer logo
Pfizer logo
Johnson & Johnson Innovative Medicine logo
Johnson & Johnson Innovative Medicine logo
Roche logo
Roche logo
Mirati Therapeutics logo
Mirati Therapeutics logo
Genentech logo
Genentech logo
Lonza logo
Lonza logo
AbbVie logo
AbbVie logo
Bausch Health logo
Bausch Health logo
Bristol Myers Squibb logo
Bristol Myers Squibb logo
Merck logo
Merck logo
Moderna logo
Moderna logo
Novartis logo
Novartis logo
Pfizer logo
Pfizer logo
Johnson & Johnson Innovative Medicine logo
Johnson & Johnson Innovative Medicine logo
Roche logo
Roche logo
Mirati Therapeutics logo
Mirati Therapeutics logo
Genentech logo
Genentech logo
Lonza logo
Lonza logo

Transform Your Program with Microstructure Science

Get started with a drug product digital twin.

Purple tablet dispersing into a fine particle cloud, illustrating drug microstructure disintegration