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The Influence of Polysaccharide Coating on the Physicochemical Parameters and Cytotoxicity of Silica Nanoparticles for Hydrophilic Biomolecules Delivery

1
CITAB—Centre for Research and Technology of Agro-Environmental and Biological Sciences, University of Trás-os-Montes e Alto Douro, Quinta de Prados, 5001-801 Vila Real, Portugal
2
Department of Biology and Environment, University of Trás-os-Montes e Alto Douro, 5001-801 Vila Real, Portugal
3
CIQUP—Research Center in Chemistry, Department of Chemistry and Biochemistry, Faculty of Sciences, Porto University, Rua do Campo Alegre, s/n, 4169-007 Porto, Portugal
4
Institute of Technology and Research, University of Tiradentes, Avenida Murilo Dantas, Farolândia, 49010-390 Aracaju, Brazil
5
Faculty of Pharmaceutical Sciences, Universidade Estadual Paulista, UNESP, Rodovia Araraquara-Jau, Km. 01, 14801-902 Araraquara, São Paulo, Brazil
6
Biopharmacy and Pharmacokinetic Unit, Pharmacy and Pharmaceutical Technology Department, School of Pharmacy, University of Barcelona, Av. Joan XXIII, s/n, 8028 Barcelona, Spain
7
Department of Pharmaceutical Technology, Faculty of Pharmacy, University of Coimbra (FFUC), Pólo das Ciências da Saúde, Azinhaga de Santa Comba, 3000-548 Coimbra, Portugal
8
CEB—Centre of Biological Engineering, University of Minho, Campus de Gualtar 4710-057 Braga, Portugal
*
Authors to whom correspondence should be addressed.
These authors contributed equally to this work.
Nanomaterials 2019, 9(8), 1081; https://doi.org/10.3390/nano9081081
Received: 5 July 2019 / Revised: 22 July 2019 / Accepted: 25 July 2019 / Published: 27 July 2019
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Abstract

The present work reports the effect of polysaccharides (chitosan and sodium alginate) on silica nanoparticles (SiNP) for hydrophilic molecules delivery taking insulin as model drug. The influence of tetraethyl orthosilicate (TEOS) and homogenization speed on SiNP properties was assessed by a 22 factorial design achieving as optimal parameters: 0.43 mol/L of TEOS and homogenization speed of 5000 rpm. SiNP mean particle size (Z-Ave) was of 256.6 nm and polydispersity index (PI) of 0.218. SiNP coated with chitosan (SiNP-CH) or sodium alginate (SiNP-SA) increased insulin association efficacy; reaching 84.6% (SiNP-SA) and 90.8% (SiNP-CH). However, coated SiNP released 50–60% of the peptide during the first 45 min at acidic environment, while uncoated SiNP only released ~30%. Similar results were obtained at pH 6.8. The low Akaike’s (AIC) values indicated that drug release followed Peppas model for SiNP-SA and second order for uncoated SiNP and SiNP-CH (pH 2.0). At pH 6.8, the best fitting was Boltzmann for Ins-SiNP. However, SiNP-CH and SiNP-SA showed a first-order behavior. Cytotoxicity of nanoparticles, assessed in Caco-2 and HepG2 cells, showed that 100 to 500 µg/mL SiNP-CH and SiNP-SA slightly decreased cell viability, comparing with SiNP. In conclusion, coating SiNP with selected polysaccharides influenced the nanoparticles physicochemical properties, the insulin release, and the effect of these nanoparticles on cell viability. View Full-Text
Keywords: silica nanoparticles; polysaccharides; insulin; hydrophilic biomolecules; factorial design; kinetic studies; cell toxicity silica nanoparticles; polysaccharides; insulin; hydrophilic biomolecules; factorial design; kinetic studies; cell toxicity
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).
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Andreani, T.; Fangueiro, J.F.; Severino, P.; de Souza, A.L.R.; Martins-Gomes, C.; Fernandes, P.M.V.; Calpena, A.C.; Gremião, M.P.; Souto, E.B.; Silva, A.M. The Influence of Polysaccharide Coating on the Physicochemical Parameters and Cytotoxicity of Silica Nanoparticles for Hydrophilic Biomolecules Delivery. Nanomaterials 2019, 9, 1081.

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