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Abstract
Several liquid lipids have been proposed to obtain nanostructured lipid carriers (NLC) with improved efficiency. An attractive strategy is the use of oils that could elicit a synergic effect with the loaded drug. In this work, different percentages (0–4% w/w) of tocopheryl acetate (TA), an oily antioxidant, were used as liquid lipid to prepare NLC loading idebenone (IDE), a synthetic antioxidant investigated for the treatment of neurodegenerative and topical diseases. The technological properties of such NLC were evaluated, as well as the interactions among lipid core components. Loading different percentages of IDE (1–4% w/w) into NLC containing TA up to 4% w/w, no significant change of mean size and polydispersity index was observed. IDE loading capacity was 4% w/w but NLC containing IDE percentages greater than 1.5% w/w showed poor stability during long-term storage. Differential scanning calorimetry analyses highlighted linear relationships between peak temperature and TA percentages, while the enthalpy variation and recrystallization index values showed that increasing the percentage of TA led to less crystalline structure of the NLC core. Therefore, NLC co-loading IDE and TA could be useful to design new delivery systems for the treatment of diseases that could benefit from the co-administration of these antioxidants.
Highlights
In the last decades, lipid nanoparticles have gained a great deal of attention in the pharmaceutical field owing to their advantages as drug delivery systems [1,2,3,4,5]
solid lipid nanoparticles (SLN) drawbacks, such as poor loading capacity and drug leakage from the nanoparticles during storage, prompted the researchers to design a second generation of lipid nanoparticles, named nanostructured lipid carriers (NLC)
The comparison between the mean size of unloaded SLN and unloaded NLC pointed out that the inclusion in the nanoparticle lipid core of percentages of tocopheryl acetate (TA) up to 3.5%
Summary
Lipid nanoparticles have gained a great deal of attention in the pharmaceutical field owing to their advantages as drug delivery systems [1,2,3,4,5]. 1990s, the first generation of lipid nanoparticles, namely solid lipid nanoparticles (SLN), was developed and investigated as carriers for the delivery of a great variety of active ingredients by different administration routes [6,7,8,9,10]. NLC with improved biological activity, in this work, NLC containing simultaneously different concentrations of IDE and TA were prepared and the influence of co-loading these antioxidants on lipid nanoparticles features such as mean sizes, polydispersity index, ζpotential, loading capacity, and long-term stability was assessed. The development of lipid nanoparticles co-loading IDE and TA could provide a promising tool for the design of new delivery systems for the treatment of neurodegenerative and topical diseases that benefit from the simultaneous administration of these two antioxidants
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