Abstract
Idebenone (IDE) is a strong antioxidant that has been proposed for the treatment of skin disorders, including skin ageing. Unfavorable physico-chemical properties make IDE a poor skin permeant where effectiveness could be improved by its loading into suitable delivery systems such as solid lipid nanoparticles (SLN) and nanostructured lipid carriers (NLC). In this work, we designed novel IDE-loaded NLC containing tocopheryl acetate (VitE) as a liquid component to obtain a synergic effect between IDE and VitE. The resulting NLC showed small particle sizes (24–42 nm), low polydispersity indices (<0.300), good stability, and were assessed for their in vitro antioxidant activity and in vivo topical effects. IDE-loaded SLN and NLC showed a high antioxidant activity in in vitro assays (DPPH and reducing power method) and provided a similar and significant protection from oxidative stress of fibroblast cells, HS-68, exposed to UV light. After a two-week topical treatment of human volunteers with gels containing IDE-loaded SLN or NLC, a similar increase in skin hydration was observed, while IDE NLC reduced skin pigmentation to a greater extent than IDE SLN. These results suggest that co-loading IDE and VitE into NLC could be a promising strategy to obtain topical formulations with improved photo-protection.
Highlights
In the last decades, solid lipid nanoparticles (SLNs) have been widely investigated as carriers for topical drug delivery [1,2,3,4,5,6,7]
Liquid lipids were mixed together with solid lipids to obtain a less packed lipid matrix, leading to a second generation of lipid nanoparticles defined as nanostructured lipid carriers (NLC) [2,3,6]
To calculate the sample crystallinity index (CI), the melting enthalpy of the lipid in the nanocarriers was expressed as a percentage of the melting enthalpy of the bulk lipid cetyl palmitate, which was considered totally crystalline as reported in previous works [22,23]
Summary
Solid lipid nanoparticles (SLNs) have been widely investigated as carriers for topical drug delivery [1,2,3,4,5,6,7]. The highly ordered structure of the solid lipid matrix of SLN could result in low incorporation of lipophilic drugs and drug leakage during storage To overcome these drawbacks, liquid lipids were mixed together with solid lipids to obtain a less packed lipid matrix, leading to a second generation of lipid nanoparticles defined as nanostructured lipid carriers (NLC) [2,3,6]. To evaluate the effect of co-loading vitamin E acetate and IDE in the matrix of lipid nanoparticles, we assessed technological properties, in vitro antioxidant activity, and cytotoxic and photo-protective effects of IDE loaded SLN and NLC on human fibroblast cells HS-68.
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