Design and characteristics of gellan gum beads for modified release of meloxicam

Abstract

The aim of the presented work was to design, formulate and evaluate the properties of low-acyl gellan macro beads with the potential application as carriers for oral delivery of meloxicam (MLX) in the prophylaxis of colorectal cancer. The beads were obtained by means of ionotropic gelation technique. Calcium chloride (1.0%, 9.0 × 10⁻² M) was used as the cross-linking agent. Nine different polymer, drug and surfactant (Tween^®80) mixtures were used for production of the beads. The quantitative compositions of the mixtures were generated with the application of the Design of Experiments (DoE) modulus from the STATISTICA Software. The prepared formulations revealed 7.2–27.0% of drug loading and 29.2–50.7% drug encapsulation efficiency. It turned out that 0.5% amount of gellan gum in the mixtures was not sufficient to obtain spherical beads. The morphology and surface of the dried beads were analyzed by SEM. Raman spectra confirmed that MLX did not undergo structural changes during production of the beads. The swelling behavior and degradation of the beads were evaluated in three simulated gastrointestinal fluids at different pH (1.2; 4.5; 6.8). The MLX in vitro release studies were conducted on USP apparatus IV, working in the open loop mode. The obtained results showed that MLX release from the dried beads was pH-dependent. The formulations obtained from mixtures containing 1.0 and 1.5% of gellan may be considered as oral dosage forms for MLX, intended to omit the stomach and release the drug in the distal parts of the gastrointestinal tract.

Keywords:

• Meloxicam
• gellan gum
• ionotropic gelation
• drug release
• Design of Experiments

Acknowledgements

The authors would like to thank professor Janina Lulek from the Department of Pharmaceutical Technology at Poznan University of Medical Sciences in Poland for scientific help and advisory. We are also very grateful to Biofarm S.A. (Poznań, Poland) for supporting our work with the free meloxicam sample and to CP Kelco (Atlanta, USA) for providing a gellan gum sample. We would like to thank Monika Kwiecińska for technical assistance during preliminary experiments. The work was partially supported by PUMS grant nos. 502-05-03314429-09983 and 502-14-03314429-09983. The DSC experiments were performed at the Department of Pharmaceutics and Biopharmaceutics at Christian Albrecht University of Kiel (Germany) as a part of a research visit.

Disclosure statement

The authors report no declarations of interest.