Toward a detailed characterization of oil adsorbates as “solid liquids”

Solid lipid formulation systems are used to overcome oral bioavailability problems of poorly water-soluble drugs. One promising process is the conversion of a liquid lipid system in a free flowing powder by use of adsorbing excipients. The aim of this study was the detailed characterization of solid–liquid interactions in oil adsorbed to Fujicalin® and Neusilin® which were manufactured by means of dual asymmetric centrifugation or conventional mortar/pestle blending. The adsorption strength of the excipients was investigated by Benchtop-NMR and ESR spectroscopy revealing the highest adsorption power for the Neusilin® products. The adsorbate production methods as well as the storage of the excipients impact their adsorption properties. Environmental scanning electron microscopy (ESEM) and confocal laser scanning microscopy (CLSM) show that dual asymmetric centrifugation leads to a smoothing of the particle surface, whereas the mortar/pestle blending results in an uneven surface and particle destruction. The oil distribution at the particles is inhomogeneous for both production methods. The micropolarity of the adsorbed oil was investigated by ESR spectroscopy and multispectral fluorescence imaging. The adsorbing process on Neusilin® leads to an increased micropolarity of the oil component. The release of the oil component in aqueous media could be verified by Benchtop-NMR and multispectral fluorescence imaging.

A detailed characterization of solid-liquid interactions in Fujicalin® and Neusilin® oil adsorbates was done by environmental scanning electron microscopy (ESEM), confocal laser scanning microscopy (CLSM), multispectral fluorescence imaging, Benchtop-NMR and ESR spectroscopy. By means of these methods it was possible to obtain information on the strength of oil-solid interactions, the micropolarity, the heterogeneity of the distribution and the release properties.Figure optionsDownload high-quality image (102 K)Download as PowerPoint slide