Thermal Analysis in the Evaluation of Solid Lipid Microparticles in the Form of Aqueous Dispersion and Fine Powder

Abstract

In the presented study, an attempt was made to investigate the most important attributes of solid lipid microparticles (SLM) using thermal analysis (DSC/TG) in order to determine the importance of this technique in the research and development of lipid microparticles. Particularly interesting in our studies were drug–lipid interactions and modifications of the SLM matrix structure induced by the production method (the hot emulsification method) and further processing (e.g., spray drying), as well as changes occurring during the stability studies. Cyclosporine A, indomethacin and spironolactone were used as model active substances incorporated into SLM. The conducted research demonstrated the significant potential of DSC/TG, especially for the analysis of SLM in the form of fine powder. The method of sample preparation, consisting of evaporation of water at room temperature, turned out to be crucial for the DSC/TG analysis of SLM dispersion. In the case of the tested SLM, the basic and usually the only observed thermal transformation in the DSC spectrum was the endothermic peak associated with the lipid forming a microsphere matrix. This peak is the main source of information about the properties and stability of the tested SLM. The obtained results show that glyceryl behenate (Compritol) is a significantly better lipid for forming lipid microparticles than stearic acid. Although thermal transformations of the incorporated drug substances are not directly visible in the DSC spectra, their impact on the SLM properties can be assessed indirectly, based on changes in the lipid melting point and the shape of the DSC and TG peaks and curves. DSC/TG studies confirmed the lack of an effect of the spray drying process on the properties of drug-loaded SLM with Compritol. Studies have also shown up to a 2-year stability of SLM with CsA.

Drug Release from Lipid Microparticles—Insights into Drug Incorporation and the Influence of Physiological Factors

“…We prepared SLM with sizes ranging from one to several micrometers ( Table 1 ), which are suitable for ocular administration, because this size is considered to be non-irritating after administration to the eye [ 32 ]. The tested lipid microparticle dispersions were also characterized by the desired long-term stability, which was described in previous studies [ 14 , 33 ].…”