Abstract: Ellagic acid (EA) is a potent antioxidant substance of natural origin characterized by poor\nbiopharmaceutical properties and low solubility in water that limit its use. The aim of the present\nstudy was to develop lipid-based nanoparticle formulations able to encapsulate EA for dermal\ndelivery. The EA-loaded nanoparticles were prepared using two different lipid compositions, namely\ntristearin/tricaprylin (NLC-EA1) and tristearin/labrasol (NLC-EA2). The influence of formulations on\nsize, entrapment efficiency, and stability of EA-loaded nanoparticles was investigated. Cryo-TEM and\nsmall-angle X-ray scattering (SAXS) analyses showed that no morphological differences are evident\namong all the types of loaded and unloaded nanostructured lipid carriers (NLCs). The macroscopic\naspect of both NLC-EA1 and NLC-EA2 did not change with time. No difference in size was\nappreciable between empty and drug-containing NLC, thus the nanoparticle diameter was not\naffected by the presence of EA and in general no variations of the diameters occurred during this time.\nThe entrapment efficiency of both EA-loaded nanoparticles was almost quantitative. In addition,\nNLC-EA1 maintained EA stability for almost two months, while NLC-EA2 up to 40 days. FRAP (Ferric\nreducing ability of plasma) assay showed an antioxidant activity around 60% for both the loaded\nNLC, as compared to the solution. Although both types of NLC are characterized by some toxicity on\nHaCaT cells, NLC-EA1 are less cytotoxic than NLC-EA2. Taken together these results demonstrated\nthat the inclusion of EA within NLC could improve the water solubility, allowing for a reduction of\nthe dosage. Moreover, both types of NLC-EA maintained a high antioxidant effect and low toxicity.
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