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

Supandeep Singh Hallan,Paolo Mariani,Elisabetta Esposito,Markus Drechsler,Rita Cortesi,Gabriella Pavoni,Anna Baldisserotto,Maddalena Sguizzato

doi:10.3390/molecules25061449

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.

Highlights

IntroductionEllagic acid (EA) (2,3,7,8-tetrahydroxy-chromeno [5,4,3-cde]chromene-5,10-dione) (Table 1) is the dimeric derivative of gallic acid and has a significant attractiveness in food supplements because of its potentially beneficial effects against a wide range of diseases [1]
The nanostructured lipid carriers (NLCs)-Ellagic acid (EA) composed as reported in Table 2, were obtained by dispersing the lipid phase in the aqueous phase under sonication [23] achieving stable and homogenous dispersions
It was demonstrated that the inclusion of EA within NLCs could improve the water solubility, allowing for a reduction of the dosage

Summary

Introduction

EA (2,3,7,8-tetrahydroxy-chromeno [5,4,3-cde]chromene-5,10-dione) (Table 1) is the dimeric derivative of gallic acid and has a significant attractiveness in food supplements because of its potentially beneficial effects against a wide range of diseases [1]. Various studies indicate that EA possesses antimutagenic, antiagenic, antioxidant, and anti-inflammatory activity in bacterial and mammalian systems [2,3,4]. Molecules 2020, 25, x FOR PEER REVIEW attractiveness in food supplements because of its potentially beneficial effects against a wide range of diseases [1].2020, Various studies indicate that EA possesses antimutagenic, antiagenic, antioxidant, and 2 of 15 Molecules. EA has proven to be an efficient skin whitener and suppressor of pigmentation. In addition to its anti-oxidant activities, EA ishas proven towards to be andifferent efficient types skin whitener of pigmentation

Objectives

Methods

Results

Conclusion