Abstract
Oxidative damage has been linked to a number of diseases. Oleuropein (OLE), a natural occurring polyphenol from olive leaves (Olea europaea L.), is known to be a potent antioxidant compound with inherent instability and compromised bioavailability. Therefore, in this work, nanostructured lipid carriers (NLCs) were proposed for OLE encapsulation to protect and improve its antioxidant efficacy. The lipid matrix, composed of olive oil and Precirol, was optimized prior to OLE encapsulation. The characterization of the optimized oleuropein-loaded NLCs (NLC-OLE) showed a mean size of 150 nm, a zeta potential of −21 mV, an encapsulation efficiency of 99.12%, sustained release profile, and improved radical scavenging activity. The cellular in vitro assays demonstrated the biocompatibility of the NLCs, which were found to improve and maintain OLE antioxidant efficacy in the A549 and CuFi-1 lung epithelial cell lines, respectively. Overall, these findings suggest a promising potential of NLC-OLE to further design a pulmonary formulation for OLE delivery in lung epithelia.
Highlights
Reactive oxygen species (ROS) have an essential role in normal cell function and signaling
In the first step of this work, Nanostructured Lipid Carriers (NLCs) were prepared through the hot melt emulsification method followed by ultrasonication (HME-Us), as previously described by our group [38]
HME-Us have gained a lot of importance after the Food and Drug Administration encouraged the use of continuous processes among the pharmaceutical industry [41] and overcome most of the limitations offered by the conventional microand nanoemulsification techniques
Summary
Reactive oxygen species (ROS) have an essential role in normal cell function and signaling. Their overproduction leads to an oxidative stress status that contributes to the development of several pathological events such as inflammation, fibrosis, genotoxicity, and carcinogenesis. Clinical evidence suggests that many lung diseases are associated with a reduced antioxidant defense, together with an increased accumulation of ROS [5]. Current strategies toward oxidative damage have been focused on the use of small ROS scavenger drugs (i.e., Edaravone, N-acetylcysteine, Cerovive®) their toxicity, together with their low clinical efficacy, has been discouraging [5,6]. Natural antioxidants have emerged as alternative or even complementary candidates with minimized toxicity
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