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Open AccessArticle

Ellagic Acid Containing Nanostructured Lipid Carriers for Topical Application: A Preliminary Study

1
Department of Chemical and Pharmaceutical Sciences, University of Ferrara, 44121 Ferrara, Italy
2
Department of Life Sciences & Biotechnology, University of Ferrara, 44121 Ferrara, Italy
3
Bavarian Polymerinstitute (BPI), University of Bayreuth, 95440 Bayreuth, Germany
4
Department of Life and Environmental Sciences, Polytechnic University of Marche, 60131 Ancona, Italy
*
Authors to whom correspondence should be addressed.
Academic Editors: Fabio Sonvico, Yangchao Luo and Domenico Lombardo
Molecules 2020, 25(6), 1449; https://doi.org/10.3390/molecules25061449 (registering DOI)
Received: 12 February 2020 / Revised: 6 March 2020 / Accepted: 18 March 2020 / Published: 23 March 2020
Ellagic acid (EA) is a potent antioxidant substance of natural origin characterized by poor biopharmaceutical properties and low solubility in water that limit its use. The aim of the present study was to develop lipid-based nanoparticle formulations able to encapsulate EA for dermal delivery. The EA-loaded nanoparticles were prepared using two different lipid compositions, namely tristearin/tricaprylin (NLC-EA1) and tristearin/labrasol (NLC-EA2). The influence of formulations on size, entrapment efficiency, and stability of EA-loaded nanoparticles was investigated. Cryo-TEM and small-angle X-ray scattering (SAXS) analyses showed that no morphological differences are evident among all the types of loaded and unloaded nanostructured lipid carriers (NLCs). The macroscopic aspect of both NLC-EA1 and NLC-EA2 did not change with time. No difference in size was appreciable between empty and drug-containing NLC, thus the nanoparticle diameter was not affected by the presence of EA and in general no variations of the diameters occurred during this time. The entrapment efficiency of both EA-loaded nanoparticles was almost quantitative. In addition, NLC-EA1 maintained EA stability for almost two months, while NLC-EA2 up to 40 days. FRAP (Ferric reducing ability of plasma) assay showed an antioxidant activity around 60% for both the loaded NLC, as compared to the solution. Although both types of NLC are characterized by some toxicity on HaCaT cells, NLC-EA1 are less cytotoxic than NLC-EA2. Taken together these results demonstrated that the inclusion of EA within NLC could improve the water solubility, allowing for a reduction of the dosage. Moreover, both types of NLC-EA maintained a high antioxidant effect and low toxicity. View Full-Text
Keywords: nanostructured lipid carriers (NLCs); lipid-based nanosystems; phytopharmaceutics; ellagic acid; antioxidant activity nanostructured lipid carriers (NLCs); lipid-based nanosystems; phytopharmaceutics; ellagic acid; antioxidant activity
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MDPI and ACS Style

Singh Hallan, S.; Sguizzato, M.; Pavoni, G.; Baldisserotto, A.; Drechsler, M.; Mariani, P.; Esposito, E.; Cortesi, R. Ellagic Acid Containing Nanostructured Lipid Carriers for Topical Application: A Preliminary Study. Molecules 2020, 25, 1449.

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