Design and characterization of sustained release ketoprofen entrapped carnauba wax microparticles

Abstract

Context: Ketoprofen is a non-steroid anti-inflammatory drug (NSAID) used in the treatment of rheumatic diseases and in mild to moderate pain. Ketoprofen has a short biological half-life and the commercially available conventional release formulations require dosages to be administered at least 2–3 times a day. Due to these characteristics, ketoprofen is a good candidate for the preparation of controlled release formulations.

Objectives: In this work, a multiparticulate-sustained release dosage form containing ketoprofen in a carnauba wax matrix was developed.

Methods: Particles were prepared by an emulsion congealing technique. System variables were optimized using fractional factorial and response surface experimental design. Characterization of the particles included size and morphology, flow rate, drug loading and in vitro drug release.

Results: Spherical particles were obtained with high drug load and sustained drug release profile. The optimized particles had an average diameter of approximately 200 µm, 50% (w/w) drug load, good flow properties and prolonged ketoprofen release for more than 24 h.

Conclusions: Carnauba wax microspheres prepared in this work represent a new multiparticulate-sustained release system for the NSAID ketoprofen, exhibiting good potential for application in further pharmaceutical processes.

Keywords::

• Carnauba wax
• microparticles
• ketoprofen
• factorial design
• sustained release
• dissolution