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Ellagic acid containing nanostructured lipid carriers for topical application: a preliminary study

DOI: 10.3390/molecules25061449 DOI Help

Authors: Supandeep Singh Hallan (University of Ferrara) , Maddalena Sguizzato (University of Ferrara) , Gabriella Pavoni (University of Ferrara) , Anna Baldisserotto (University of Ferrara) , Markus Drechsler (University of Bayreuth) , Paolo Mariani (Polytechnic University of Marche) , Elisabetta Esposito (University of Ferrara) , Rita Cortesi (University of Ferrara)
Co-authored by industrial partner: No

Type: Journal Paper
Journal: Molecules , VOL 25

State: Published (Approved)
Published: March 2020

Open Access Open Access

Abstract: 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.

Journal Keywords: nanostructured lipid carriers (NLCs); lipid-based nanosystems; phytopharmaceutics; ellagic acid; antioxidant activity

Subject Areas: Chemistry, Biology and Bio-materials, Medicine

Instruments: B21-High Throughput SAXS