Nanostructured Lipid Carriers Aimed to the Ocular Delivery of Mangiferin: In Vitro Evidence

Although mangiferin (MGN) is a natural antioxidant that could be a good candidate for the treatment of ocular diseases, its use in ophthalmology is strongly compromised due to its high lipophilicity. Its encapsulation in nanostructured lipid carriers (NLC) seems to be an interesting strategy for improving its ocular bioavailability. As reported in our previous work, MGN–NLC showed high ocular compatibility and fulfilled the nanotechnological requirements needed for ocular delivery. The aim of the present work was to investigate, in vitro and ex vivo, the capability of MGN–NLC to act as a potential drug delivery system for MGN ocular administration. The data obtained in vitro on arising retinal pigment epithelium cells (ARPE-19) did not show cytotoxic effects for blank NLC and MGN–NLC; likewise, MGN–NLC showed the maintenance of the antioxidant role of MGN by mitigating ROS (Reactive Oxygen Species) formation and GSH (glutathione) depletion induced by H₂O₂. In addition, the capacity of MGN-released to permeate through and accumulate into the ocular tissues was confirmed ex vivo using bovine corneas. Finally, the NLC suspension has been formulated as a freeze-dried powder using mannitol at a concentration of 3% (w/v) in order to optimize its storage for long periods of time. All this evidence suggests a potential application of MGN–NLC in the treatment of oxidative stress-related ocular diseases.

2.1. Materials

Compritol 888 ATO was obtained from Gattefossè (Milan, Italy), oil Miglyol 812 was provided by Eigenmann & Veronelli S.p.A. (Milan, Italy) and Lutrol F68 was purchased from BASF ChemTrade GmbH (Burgbernheim, Germany). Mangiferin, Phosphate Buffered Saline (PBS commercial 10×) and all solvents were purchased from Merck (Milan, Italy). Ultrapure water (resistivity > 18.2 MΩ·cm) was obtained by reverse osmosis (Milli-Q, Millipore Iberica, Madrid, Spain). The ARPE 19 cell line was purchased from ATCC, and bromide 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium (MTT), dimethyl sulfoxide (DMSO), sulfhydryl reagent 5,5′-dithio-bis (2-nitrobenzoic acid) (DTNB) and 2′,7′- dichlorofluorescein diacetate (DCFH-DA) were purchased from Sigma–Merk Life Science, Milan, IT.

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Santonocito, D.; Barbagallo, I.; Distefano, A.; Sferrazzo, G.; Vivero-Lopez, M.; Sarpietro, M.G.; Puglia, C. Nanostructured Lipid Carriers Aimed to the Ocular Delivery of Mangiferin: In Vitro Evidence. Pharmaceutics 2023, 15, 951.
https://doi.org/10.3390/pharmaceutics15030951

excipients formulation