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Open AccessArticle

Chitosan-Coated Nanoparticles: Effect of Chitosan Molecular Weight on Nasal Transmucosal Delivery

1
Programa de Pós-Graduação em Ciências Farmacêuticas, Universidade Federal do Rio Grande do Sul, Porto Alegre 90610-000, Brazil
2
Food and Drug Department, University of Parma, Parco Area delle Scienze 27/a, 43124 Parma, Italy
3
Programa de Pós-Graduação em Biociências, Universidade Federal de Ciências da Saúde de Porto Alegre, Porto Alegre RS 900500-170, Brazil
4
Department of Life Sciences and Biotechnology, University of Ferrara, Via Fossato di Mortara 17/19, 44121 Ferrara, Italy
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Programa de Pós-Graduação em Ciências Fisiológicas, Universidade Federal do Rio Grande, Rio Grande RS 96203-000, Brazil
6
Departamento de Química Orgânica, Instituto de Química, Universidade Federal do Rio Grande do Sul, Porto Alegre 91501-970, Brazil
*
Author to whom correspondence should be addressed.
Pharmaceutics 2019, 11(2), 86; https://doi.org/10.3390/pharmaceutics11020086
Received: 1 February 2019 / Revised: 14 February 2019 / Accepted: 15 February 2019 / Published: 18 February 2019
(This article belongs to the Special Issue Transmucosal Absorption Enhancers in the Drug Delivery Field)
Drug delivery to the brain represents a challenge, especially in the therapy of central nervous system malignancies. Simvastatin (SVT), as with other statins, has shown potential anticancer properties that are difficult to exploit in the central nervous system (CNS). In the present work the physico–chemical, mucoadhesive, and permeability-enhancing properties of simvastatin-loaded poly-ε-caprolactone nanocapsules coated with chitosan for nose-to-brain administration were investigated. Lipid-core nanocapsules coated with chitosan (LNCchit) of different molecular weight (MW) were prepared by a novel one-pot technique, and characterized for particle size, surface charge, particle number density, morphology, drug encapsulation efficiency, interaction between surface nanocapsules with mucin, drug release, and permeability across two nasal mucosa models. Results show that all formulations presented adequate particle sizes (below 220 nm), positive surface charge, narrow droplet size distribution (PDI < 0.2), and high encapsulation efficiency. Nanocapsules presented controlled drug release and mucoadhesive properties that are dependent on the MW of the coating chitosan. The results of permeation across the RPMI 2650 human nasal cell line evidenced that LNCchit increased the permeation of SVT. In particular, the amount of SVT that permeated after 4 hr for nanocapsules coated with low-MW chitosan, high-MW chitosan, and control SVT was 13.9 ± 0.8 μg, 9.2 ± 1.2 µg, and 1.4 ± 0.2 µg, respectively. These results were confirmed by SVT ex vivo permeation across rabbit nasal mucosa. This study highlighted the suitability of LNCchit as a promising strategy for the administration of simvastatin for a nose-to-brain approach for the therapy of brain tumors. View Full-Text
Keywords: nasal permeability; nose-to-brain; simvastatin; nanocapsules; mucoadhesion; CNS disorders; chitosan nasal permeability; nose-to-brain; simvastatin; nanocapsules; mucoadhesion; CNS disorders; chitosan
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MDPI and ACS Style

Bruinsmann, F.A.; Pigana, S.; Aguirre, T.; Dadalt Souto, G.; Garrastazu Pereira, G.; Bianchera, A.; Tiozzo Fasiolo, L.; Colombo, G.; Marques, M.; Raffin Pohlmann, A.; Stanisçuaski Guterres, S.; Sonvico, F. Chitosan-Coated Nanoparticles: Effect of Chitosan Molecular Weight on Nasal Transmucosal Delivery. Pharmaceutics 2019, 11, 86.

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