Journal
NANOMEDICINE-NANOTECHNOLOGY BIOLOGY AND MEDICINE
Volume 6, Issue 6, Pages 745-752Publisher
ELSEVIER
DOI: 10.1016/j.nano.2010.06.006
Keywords
Antioxidant; Idebenone; Nanoparticles; Chitosan; N-Carboxymethylchitosan; Spray-dryer; Stability; Mucous membrane irritation
Funding
- National Council of Scientific and Technological Development-CNPq [5169/2005-7, 472264/07-9]
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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 mu m, 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 Editor: Chitosan and N-carboxymethylchitosan nanoparticles have potential roles as carriers for hydrophobic and irritative drugs such as the antioxidant idebenone for topical or nasal use. (c) 2010 Elsevier Inc. All rights reserved.
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