Coated formulations: New insights into the release mechanism and changes in the film properties with a novel release cell

The effect of the blend ratio of water-insoluble ethyl cellulose (EC) and water-soluble hydroxypropyl cellulose (HPC-LF), on the properties of sprayed films and on the drug release mechanism of formulations coated with the material was investigated. When the original HPC-LF content exceeded 22%, both the amount of HPC-LF leached out and the water permeability of the films increased drastically when they were immersed in a phosphate buffer solution. The release mechanism of potassium nitrate through EC/HPC-LF films containing 20, 24 and 30% HPC-LF was elucidated in a new release cell equipped with a manometer to measure the pressure build-up inside the cell. A lag phase in the release accompanied by a pressure build-up was observable in all the experiments showing that all the films were initially semi-permeable to KNO3. However, pressure data revealed that films with 30% HPC-LF became permeable to KNO3 during the release process due to HPC-LF leaching. Importantly, the blend ratio influenced not only the release rate (which increased as the amount of HPC-LF increased), and the lag time (which increased as the amount of HPC-LF decreased), but also the release mechanism, which changed from osmotic pumping to diffusion as the amount of HPC-LF increased.

Graphical abstractThe release cell simulates a coated formulation. The release mechanism (osmotic pumping and/or diffusion) and changes in the coating properties are accurately studied by acquiring pressure and release data simultaneously.Figure optionsDownload full-size imageDownload as PowerPoint slide