Preprint Article Version 1 This version is not peer-reviewed

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

Version 1 : Received: 1 February 2019 / Approved: 4 February 2019 / Online: 4 February 2019 (13:27:10 CET)

A peer-reviewed article of this Preprint also exists.

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

Journal reference: Pharmaceutics 2019, 11, 86
DOI: 10.3390/pharmaceutics11020086

Abstract

Drug delivery to the brain represents a challenge especially in the therapy of central nervous system malignancies. Simvastatin (SVT), as other statins, has shown potential anticancer properties that are difficult to exploit in the 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 different molecular weight (MW) chitosans (LNCchit) prepared by a novel one-pot technique were 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 present adequate particle size (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 dependent on the MW of the coating chitosan. The results of permeation across RPMI 2650 human nasal cell line evidenced that LNCchit increased the permeation of SVT. In particular, the amount of SVT permeated after 4h for nanocapsules coated with low MW chitosan, high MW chitosan and control SVT was 13.91 ± 0.78 µg, 9.15 ± 1.23 µg and 1.42 ± 0.21 µg respectively. These results were confirmed by the SVT ex vivo permeation across rabbit nasal mucosa. This study highlighted the suitability of LNCchit as promising strategy for the administration of simvastatin for a nose-to-brain approach for the therapy of brain tumors.

Subject Areas

nasal permeability; nose-to-brain; simvastatin; nanocapsules; mucoadhesion; CNS disorders; chitosan

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