Influence of stearic acid and beeswax as solid lipid matrix of lipid nanoparticles containing tacrolimus

Lipid nanoparticles, both solid lipid nanoparticles and nanostructured lipid carriers (NLC), containing tacrolimus (FK) were obtained by solvent diffusion method associated with ultrasonication using stearic acid (SA) or beeswax as solid lipid. The oleic acid was used as liquid lipid in the NLC. Lipid nanoparticles were characterized by determining the drug loading, particle size, polydispersity index (PDI) and zeta potential (ZP). Analysis by differential scanning calorimetry and X-ray diffraction were performed. Lipid nanoparticles presented nano-sized from 139 to 275 nm. The PDI results show the particles present from 0.3 to 0.5, and ZP was higher than |25| mV. Drug loading ranged of 2.3-3.2%. SA nanoparticles presented better ZP, average size and distribution. However, beeswax nanoparticles showed higher drug loading. Results suggest there are no incompatibilities between FK and the raw materials. Polymorphic modifications were not observed. The results presented show that lipid nanoparticles using both lipids were successfully obtained and may represent promising delivery system of FK in topical formulations.