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Article

How Can Biomolecules Improve Mucoadhesion of Oral Insulin? A Comprehensive Insight using Ex-Vivo, In Silico, and In Vivo Models

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Research Institute for Medicines (iMed.ULisboa), Faculty of Pharmacy, Universidade de Lisboa, 1649-003 Lisboa, Portugal
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Faculdade de Medicina Veterinária, Universidade Lusófona de Humanidades e Tecnologias/DNAtech Laboratório Veterinário, 1749-024 Lisboa, Portugal
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Department of Pharmacy and Pharmacology, School of Therapeutic Sciences, Faculty of Health Sciences, University of the Witwatersrand, Johannesburg 2193, South Africa
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JCS. Dr. Joaquim Chaves, Laboratório de Análises Clínicas, 1495-068 Miraflores-Algés, Portugal
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Centro de Química Estrutural, Departamento de Engenharia Química, Instituto Superior Técnico, Universidade de Lisboa, Av. Rovisco Pais, 1049-001 Lisboa, Portugal
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Centro de Estudos do Ambiente e do Mar (CESAM), Faculdade de Ciências, Universidade de Lisboa, Campo Grande, 1749-016 Lisboa, Portugal
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CEDOC, NOVA Medical School/Faculdade de Ciências Médicas (NMS/FCM), Universidade Nova de Lisboa, 1150-082 Lisboa, Portugal
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Ciências Funcionais e Alvos Terapêuticos, NOVA Medical School, Faculdade de Ciências Médicas (NMS|FCM), Universidade Nova de Lisboa, 1169-056 Lisboa, Portugal
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Departamento de Física, Faculdade de Ciências e Tecnologia, Universidade Nova de Lisboa, 2829-516 Caparica, Portugal
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DREAMS, Universidade Lusófona de Humanidades e Tecnologias, Campo Grande 376, 1749-024 Lisboa, Portugal
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Pharmacology & Pharmaceutical Care, Faculty of Pharmacy, Universidade de Coimbra, 3000-548 Coimbra, Portugal
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Coimbra Institute for Clinical and Biomedical Research (iCBR), University de Coimbra, 3000-370 Coimbra, Portugal
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IBEB, Biophysics & Biomedical Engineering, Faculdade de Ciências, Universidade de Lisboa, 1749-016 Lisboa, Portugal
*
Author to whom correspondence should be addressed.
These authors contributed equally to this work.
Biomolecules 2020, 10(5), 675; https://doi.org/10.3390/biom10050675
Received: 30 March 2020 / Revised: 14 April 2020 / Accepted: 22 April 2020 / Published: 27 April 2020
(This article belongs to the Special Issue Marine-Derived Biomolecules)
Currently, insulin can only be administered through the subcutaneous route. Due to the flaws associated with this route, it is of interest to orally deliver this drug. However, insulin delivered orally has several barriers to overcome as it is degraded by the stomach’s low pH, enzymatic content, and poor absorption in the gastrointestinal tract. Polymers with marine source like chitosan are commonly used in nanotechnology and drug delivery due to their biocompatibility and special features. This work focuses on the preparation and characterization of mucoadhesive insulin-loaded polymeric nanoparticles. Results showed a suitable mean size for oral administration (<600 nm by dynamic laser scattering), spherical shape, encapsulation efficiency (59.8%), and high recovery yield (80.6%). Circular dichroism spectroscopy demonstrated that protein retained its secondary structure after encapsulation. Moreover, the mucoadhesive potential of the nanoparticles was assessed in silico and the results, corroborated with ex-vivo experiments, showed that using chitosan strongly increases mucoadhesion. Besides, in vitro and in vivo safety assessment of the final formulation were performed, showing no toxicity. Lastly, the insulin-loaded nanoparticles were effective in reducing diabetic rats’ glycemia. Overall, the coating of insulin-loaded nanoparticles with chitosan represents a potentially safe and promising approach to protect insulin and enhance peroral delivery. View Full-Text
Keywords: marine-derived biomolecules; diabetes mellitus; insulin; mucoadhesion; nanoparticle; oral delivery marine-derived biomolecules; diabetes mellitus; insulin; mucoadhesion; nanoparticle; oral delivery
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MDPI and ACS Style

Amaral, M.; Martins, A.S.; Catarino, J.; Faísca, P.; Kumar, P.; Pinto, J.F.; Pinto, R.; Correia, I.; Ascensão, L.; Afonso, R.A.; Gaspar, M.M.; Charmier, A.J.; Figueiredo, I.V.; Reis, C.P. How Can Biomolecules Improve Mucoadhesion of Oral Insulin? A Comprehensive Insight using Ex-Vivo, In Silico, and In Vivo Models. Biomolecules 2020, 10, 675. https://doi.org/10.3390/biom10050675

AMA Style

Amaral M, Martins AS, Catarino J, Faísca P, Kumar P, Pinto JF, Pinto R, Correia I, Ascensão L, Afonso RA, Gaspar MM, Charmier AJ, Figueiredo IV, Reis CP. How Can Biomolecules Improve Mucoadhesion of Oral Insulin? A Comprehensive Insight using Ex-Vivo, In Silico, and In Vivo Models. Biomolecules. 2020; 10(5):675. https://doi.org/10.3390/biom10050675

Chicago/Turabian Style

Amaral, Mariana, Ana Sofia Martins, José Catarino, Pedro Faísca, Pradeep Kumar, João F. Pinto, Rui Pinto, Isabel Correia, Lia Ascensão, Ricardo A. Afonso, M. Manuela Gaspar, Adília J. Charmier, Isabel Vitória Figueiredo, and Catarina Pinto Reis. 2020. "How Can Biomolecules Improve Mucoadhesion of Oral Insulin? A Comprehensive Insight using Ex-Vivo, In Silico, and In Vivo Models" Biomolecules 10, no. 5: 675. https://doi.org/10.3390/biom10050675

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