Abstract
Follicular targeting has gained more attention in recent decades, due to the possibility of obtaining a depot effect in topical administration and its potential as a tool to treat hair follicle-related diseases. Lipid core ethyl cellulose lipomers were developed and optimized, following which characterization of their physicochemical properties was carried out. Dexamethasone was encapsulated in the lipomers (size, 115 nm; polydispersity, 0.24; zeta-potential (Z-potential), +30 mV) and their in vitro release profiles against dexamethasone in solution were investigated by vertical diffusion Franz cells. The skin biodistribution of the fluorescent-loaded lipomers was observed using confocal microscopy, demonstrating the accumulation of both lipomers and fluorochromes in the hair follicles of pig skin. To confirm this fact, immunofluorescence of the dexamethasone-loaded lipomers was carried out in pig hair follicles. The anti-inflammatory (via TNFα) efficacy of the dexamethasone-loaded lipomers was demonstrated in vitro in an HEK001 human keratinocytes cell culture and the in vitro cytotoxicity of the nanoformulation was investigated.
Highlights
Nanoparticles are pharmaceutical forms that are used to improve the efficacy and bioavailability of different poorly water-soluble active ingredients
The pharmaceutical interest of cellulose derivatives has increased in recent years, due to economic factors and as they originate from renewable resources [24]
EC was selected as the lipid core polymeric nanocapsules (LPNCs) polymer, as it has been approved by the Food and Drug Administration (FDA) for medical and food applications, and it has shown good biocompatibility in ocular drug delivery systems [25,26,27]
Summary
Nanoparticles are pharmaceutical forms that are used to improve the efficacy and bioavailability of different poorly water-soluble active ingredients. Lipomers are a promising drug delivery system to improve the therapeutical balance of DEX in AA treatment, due to possible accumulation in the pilosebaceous unit, where the disease takes place, and under the hypothesis that the lipid nucleus increases the loading capacity. This fact leads to a higher drug concentration in the LPNCs, compared with similar particles without the lipidic core, for which the DEX loading capacity was about 1–2% [16]. LPNCs have potential as a tool for the topical treatment of AA and other inflammatory skin diseases
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