Antioxidant idebenone-loaded nanoparticles based on chitosan and N-carboxymethylchitosan

Nanoparticles based on chitosan (Ch) and N-carboxymethylchitosan (N-CMCh) cross-linked with tripolyphosphate (TPP) were developed by co-drying with idebenone in different polymer-to-drug ratios (1.3:1 to 16:1) with 20% (wt/wt) colloidal silicon dioxide and tripolyphosphate (0.2 mg/mL). At high ratios (8:1 and 16:1) the spray-dried powder showed spherical and dense particles with a size close to 1 μm, allowing almost complete drug coating by the polymeric system and a high efficiency of drug incorporation (>90% and >80%, for Ch and N-CMCh, respectively). The nanoparticles showed a 10-fold increase of drug stability in comparison with free drug and preserved antioxidant activity in vitro. Compared with the severely irritative free form of idebenone, the nanoparticle formulation showed decreased mucous membrane irritation. These results revealed the potential of Ch and N-CMCh nanoparticles as carriers for a hydrophobic and irritative drug such as idebenone for topical or nasal use.From the Clinical EditorChitosan and N-carboxymethylchitosan nanoparticles have potential roles as carriers for hydrophobic and irritative drugs such as the antioxidant idebenone for topical or nasal use.

Graphical AbstractThe nanoparticles of Chitosan (Ch) or N-carboxymethylchitosan (N-CMCh) (< 1 μm) showed a high increase of antioxidant Idebenone (IDB) stability in comparison with the free drug and preserved its antioxidant activity in vitro. Compared to the severely irritative free form of IDB, the nanoparticles showed decreased mucous-membrane irritation. These results revealed the potential of Ch and N-CMCh nanoparticles as carrier for a hydrophobic and irritative drug such as idebenone for topical or nasal use.Figure optionsDownload high-quality image (306 K)Download as PowerPoint slide