Drug loading to mesoporous silica carriers by solvent evaporation: A comparative study of amorphization capacity and release kinetics

The sorption of poorly aqueous soluble active pharmaceutical ingredients (API) to mesoporous silica carriers is an increasingly common formulation strategy for dissolution rate enhancement for this challenging group of substances. However, the success of this approach for a particular API depends on an array of factors including the properties of the porous carrier, the loading method, or the attempted mass fraction of the API. At present, there is no established methodology for the rational selection of these parameters. In the present work, we report a systematic comparison of four well-characterised silica carriers and seven APIs loaded by the same solvent evaporation method. In each case, we find the maximum amorphization capacity by x-ray powder diffraction analysis and measure the in vitro drug release kinetics. For a selected case, we also demonstrate the potential for bioavailability enhancement by a permeation essay.

Automated summary

This study systematically compared the sorption of poorly aqueous soluble active pharmaceutical ingredients to different mesoporous silica carriers, and identified potential pathways for enhancing bioavailability through the rational selection of parameters.