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.
Amorim
Clarissa de M
Cde M
Núcleo de Investigações Químico-Farmacêuticas (Niqfar), Programa de Mestrado em Ciências Farmacêuticas, Universidade do Vale do Itajaí (UNIVALI), Itajaí, Santa Catarina, Brazil.
Couto
Angélica G
AG
Netz
Daisy J A
DJ
de Freitas
Rilton A
RA
Bresolin
Tania M B
TM
D000975:Antioxidants / Q000737:chemistry*; D048271:Chitosan / Q000737:chemistry*; D004337:Drug Carriers / Q000737:chemistry*; D008855:Microscopy, Electron, Scanning; D053758:Nanoparticles / Q000737:chemistry* / Q000648:ultrastructure; D010316:Particle Size; D013055:Spectrophotometry, Infrared; D014451:Ubiquinone / Q000031:analogs & derivatives* / Q000737:chemistry
D000975:Antioxidants; D004337:Drug Carriers; D014451:Ubiquinone; D048271:Chitosan; C036619:idebenone