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Volume 22
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10.3390/ijms222413258
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Article

In Vitro Comparative Study of Solid Lipid and PLGA Nanoparticles Designed to Facilitate Nose-to-Brain Delivery of Insulin

by
Hussein Akel
1,
Ildikó Csóka
1,
Rita Ambrus
1,
Alexandra Bocsik
2,
Ilona Gróf
2,
Mária Mészáros
2,
Anikó Szecskó
2,
Gábor Kozma
3,
Szilvia Veszelka
2,
Mária A. Deli
2,
Zoltán Kónya
3 and
Gábor Katona
1,*
1
Faculty of Pharmacy, Institute of Pharmaceutical Technology and Regulatory Affairs, University of Szeged, Eötvös Str. 6, H-6720 Szeged, Hungary
2
Biological Research Centre, Institute of Biophysics, Temesvári Blvd. 62, H-6726 Szeged, Hungary
3
Department of Applied & Environmental Chemistry, Faculty of Science and Informatics, Rerrich Béla Sqr. 1, H-6720 Szeged, Hungary
*
Author to whom correspondence should be addressed.
Int. J. Mol. Sci. 2021, 22(24), 13258; https://doi.org/10.3390/ijms222413258
Submission received: 4 November 2021 / Revised: 3 December 2021 / Accepted: 6 December 2021 / Published: 9 December 2021
(This article belongs to the Special Issue Nanoparticles in CNS Diseases)
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Abstract

The brain insulin metabolism alteration has been addressed as a pathophysiological factor underlying Alzheimer’s disease (AD). Insulin can be beneficial in AD, but its macro-polypeptide nature negatively influences the chances of reaching the brain. The intranasal (IN) administration of therapeutics in AD suggests improved brain-targeting. Solid lipid nanoparticles (SLNs) and poly(lactic-co-glycolic acid) nanoparticles (PLGA NPs) are promising carriers to deliver the IN-administered insulin to the brain due to the enhancement of the drug permeability, which can even be improved by chitosan-coating. In the present study, uncoated and chitosan-coated insulin-loaded SLNs and PLGA NPs were formulated and characterized. The obtained NPs showed desirable physicochemical properties supporting IN applicability. The in vitro investigations revealed increased mucoadhesion, nasal diffusion, and drug release rate of both insulin-loaded nanocarriers over native insulin with the superiority of chitosan-coated SLNs. Cell-line studies on human nasal epithelial and brain endothelial cells proved the safety IN applicability of nanoparticles. Insulin-loaded nanoparticles showed improved insulin permeability through the nasal mucosa, which was promoted by chitosan-coating. However, native insulin exceeded the blood-brain barrier (BBB) permeation compared with nanoparticulate formulations. Encapsulating insulin into chitosan-coated NPs can be beneficial for ensuring structural stability, enhancing nasal absorption, followed by sustained drug release.
Keywords: insulin; nose-to-brain delivery; solid lipid nanoparticles; PLGA nanoparticles; chitosan-coating; mucoadhesion; nasal mucosa permeability; blood-brain barrier permeability insulin; nose-to-brain delivery; solid lipid nanoparticles; PLGA nanoparticles; chitosan-coating; mucoadhesion; nasal mucosa permeability; blood-brain barrier permeability
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MDPI and ACS Style

Akel, H.; Csóka, I.; Ambrus, R.; Bocsik, A.; Gróf, I.; Mészáros, M.; Szecskó, A.; Kozma, G.; Veszelka, S.; Deli, M.A.; et al. In Vitro Comparative Study of Solid Lipid and PLGA Nanoparticles Designed to Facilitate Nose-to-Brain Delivery of Insulin. Int. J. Mol. Sci. 2021, 22, 13258. https://doi.org/10.3390/ijms222413258

AMA Style

Akel H, Csóka I, Ambrus R, Bocsik A, Gróf I, Mészáros M, Szecskó A, Kozma G, Veszelka S, Deli MA, et al. In Vitro Comparative Study of Solid Lipid and PLGA Nanoparticles Designed to Facilitate Nose-to-Brain Delivery of Insulin. International Journal of Molecular Sciences. 2021; 22(24):13258. https://doi.org/10.3390/ijms222413258

Chicago/Turabian Style

Akel, Hussein, Ildikó Csóka, Rita Ambrus, Alexandra Bocsik, Ilona Gróf, Mária Mészáros, Anikó Szecskó, Gábor Kozma, Szilvia Veszelka, Mária A. Deli, and et al. 2021. "In Vitro Comparative Study of Solid Lipid and PLGA Nanoparticles Designed to Facilitate Nose-to-Brain Delivery of Insulin" International Journal of Molecular Sciences 22, no. 24: 13258. https://doi.org/10.3390/ijms222413258

APA Style

Akel, H., Csóka, I., Ambrus, R., Bocsik, A., Gróf, I., Mészáros, M., Szecskó, A., Kozma, G., Veszelka, S., Deli, M. A., Kónya, Z., & Katona, G. (2021). In Vitro Comparative Study of Solid Lipid and PLGA Nanoparticles Designed to Facilitate Nose-to-Brain Delivery of Insulin. International Journal of Molecular Sciences, 22(24), 13258. https://doi.org/10.3390/ijms222413258

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