Abstract

The aim of this study was to explore the potential of novel nanoparticles (NPs)intended for topical administration of the hydrophilic antioxidant Glutathione and thelipophilic Idebenone. Glutathione was introduced into the NPs using two approaches: i)covalently bonded to Chitosan; ii) physically complexed with Idebenone andSulfobutylether-?-cyclodextrin.Methodology: NPs wereformulated using the ionic gelation technique, by dissolving thepolysaccharide-forming matrix (Chitosan, Glycol chitosan, Glutathionyl Chitosan) in wateror in slightly acidic solution. Idebenone was physically entrapped whereas glutathione waseither physically entrapped or covalently bonded to chitosan.Physicochemical characterization of the resulting NPs included size, zeta potentialmeasurements, antioxidant association efficiency, differential scanning calorimetry (DSC)and stability studies. Antioxidants in vitro release from the most stable NPs was assessedwith Franz diffusion cells, and the in vitro antioxidant activity was evaluated by the 2,2diphenyl-1-picrylhydrazyl(DPPH) radical test. NP cytotoxicity was assessed onimmortalized human keratinocytes (HaCaT) cell line.Results: The NPs showed smaller particle size in acidic solution than in aqueousmedium, whereas zeta potential values were always positive, irrespective of the medium.Stability studies led to the choice of the aqueous formulation where Glutathione wascovalently bonded to Chitosan for this study. DSC highlighted amorphization of Idebenonein these NPs. In vitro release studies showed that only Idebenone was released from theNPs. The antioxidant activity test revealed a strong effect (close to 100%) of Idebenoneloaded into NPs while its aqueous solution showed no activity. No cytotoxicity in humankeratinocytes was observed for the investigated NPs.Conclusion: The results of this study suggest that Idebenone can be loaded into ahydrophilic delivery system without organic solvents, often used for its solubilization,possessing high antioxidant activity. Therefore, these nanocarriers represent a promisingstrategy for the design of formulations for topical treatments with antioxidants.

Autore Pugliese

• Fini Paola

Tutti gli autori

• Montenegro L.; Trapani A.; Fini P.; Mandracchia D. ;Latrofa A.;Cioffi N.; Chiarantini L.; Picceri G.G.; ;Brundu S.; Puglisi G.

Titolo volume/Rivista

British journal of pharmaceutical research

Anno di pubblicazione

2014

ISSN

2231-2919

ISBN

Non Disponibile

Numero di citazioni Wos

Nessuna citazione

Ultimo Aggiornamento Citazioni

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Numero di citazioni Scopus

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Ultimo Aggiornamento Citazioni

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Settori ERC

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Codici ASJC

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