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Article

Zein-Based Nanoparticles as Oral Carriers for Insulin Delivery

1
Department of Chemistry and Pharmaceutical Technology, University of Navarra, C/Irunlarrea 1, 31008 Pamplona, Spain
2
Center for Nutrition Research, School of Pharmacy and Nutrition, University of Navarra, C/Irunlarrea 1, 31008 Pamplona, Spain
3
Department of Chemistry, University of Navarra, C/Irunlarrea 1, 31008 Pamplona, Spain
4
i3S, Instituto de Investigação e Inovação em Saúde, Alfredo Allen 208, 4200-180 Porto, Portugal
5
CESPU—Instituto de Investigação e Formação Avançada em Ciências e Tecnologias da Saúde, 4585-116 Gandra, Portugal
*
Author to whom correspondence should be addressed.
Academic Editors: Donato Cosco and Agnese Gagliardi
Pharmaceutics 2022, 14(1), 39; https://doi.org/10.3390/pharmaceutics14010039
Received: 26 November 2021 / Revised: 21 December 2021 / Accepted: 22 December 2021 / Published: 24 December 2021
Zein, the major storage protein from corn, has a GRAS (Generally Regarded as Safe) status and may be easily transformed into nanoparticles, offering significant payloads for protein materials without affecting their stability. In this work, the capability of bare zein nanoparticles (mucoadhesive) and nanoparticles coated with poly(ethylene glycol) (mucus-permeating) was evaluated as oral carriers of insulin (I-NP and I-NP-PEG, respectively). Both nanocarriers displayed sizes of around 270 nm, insulin payloads close to 80 µg/mg and did not induce cytotoxic effects in Caco-2 and HT29-MTX cell lines. In Caenorhabditis elegans, where insulin decreases fat storage, I-NP-PEG induced a higher reduction in the fat content than I-NP and slightly lower than the control (Orlistat). In diabetic rats, nanoparticles induced a potent hypoglycemic effect and achieved an oral bioavailability of 4.2% for I-NP and 10.2% for I-NP-PEG. This superior effect observed for I-NP-PEG would be related to their capability to diffuse through the mucus layer and reach the surface of enterocytes (where insulin would be released), whereas the mucoadhesive I-NP would remain trapped in the mucus, far away from the absorptive epithelium. In summary, PEG-coated zein nanoparticles may be an interesting device for the effective delivery of proteins through the oral route. View Full-Text
Keywords: zein; insulin; nanoparticles; mucus-permeating; poly(ethylene glycol); oral delivery zein; insulin; nanoparticles; mucus-permeating; poly(ethylene glycol); oral delivery
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MDPI and ACS Style

Reboredo, C.; González-Navarro, C.J.; Martínez-López, A.L.; Martínez-Ohárriz, C.; Sarmento, B.; Irache, J.M. Zein-Based Nanoparticles as Oral Carriers for Insulin Delivery. Pharmaceutics 2022, 14, 39. https://doi.org/10.3390/pharmaceutics14010039

AMA Style

Reboredo C, González-Navarro CJ, Martínez-López AL, Martínez-Ohárriz C, Sarmento B, Irache JM. Zein-Based Nanoparticles as Oral Carriers for Insulin Delivery. Pharmaceutics. 2022; 14(1):39. https://doi.org/10.3390/pharmaceutics14010039

Chicago/Turabian Style

Reboredo, Cristian, Carlos J. González-Navarro, Ana Luisa Martínez-López, Cristina Martínez-Ohárriz, Bruno Sarmento, and Juan M. Irache. 2022. "Zein-Based Nanoparticles as Oral Carriers for Insulin Delivery" Pharmaceutics 14, no. 1: 39. https://doi.org/10.3390/pharmaceutics14010039

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