Preparation, Characterization and Evaluation of Guar Films Impregnated with Relaxing Peptide Loaded into Chitosan Microparticles

Background: Biological molecules such as therapeutic proteins and peptides have provided ample opportunities for further improvements in health and wellbeing. However, such biomacromolecules face stability challenges regarding premature processing and digestion, whenever any enteric delivery route i...

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Autores principales: Patrícia Batista, Pedro M. Castro, Ana Raquel Madureira, Bruno Sarmento, Manuela Pintado
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Lenguaje:EN
Publicado: MDPI AG 2021
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spelling oai:doaj.org-article:d4ce6b091693428d94a20f19796005d42021-11-11T14:58:59ZPreparation, Characterization and Evaluation of Guar Films Impregnated with Relaxing Peptide Loaded into Chitosan Microparticles10.3390/app112198492076-3417https://doaj.org/article/d4ce6b091693428d94a20f19796005d42021-10-01T00:00:00Zhttps://www.mdpi.com/2076-3417/11/21/9849https://doaj.org/toc/2076-3417Background: Biological molecules such as therapeutic proteins and peptides have provided ample opportunities for further improvements in health and wellbeing. However, such biomacromolecules face stability challenges regarding premature processing and digestion, whenever any enteric delivery route is considered. Hence, oral guar films entrapping peptide-containing chitosan microparticles have been developed as a new delivery system to carry and protect therapeutic relaxing peptides. Results: The composite films were characterized regarding physicochemical properties using FTIR as well as peptide encapsulation efficiency, cytotoxicity, and peptide permeability through buccal and intestinal cell-based models. The composite films with 0.18% (<i>w/w</i>) of peptide demonstrated ca. 0.63% of peptide loading efficiency into the chitosan microparticles and to be safe for buccal and intestinal epithelial cells up to 24 h of contact. The permeability assays through TR146 cells to mimic buccal mucosa epithelium and Caco-2/HT29-MTX to mimic duodenum conditions showed that the incorporation of peptide chitosan microparticles into guar-gum oral films offered a faster permeability, when compared with the free peptide and peptide-chitosan-microparticles-loaded chitosan. Conclusion: This study suggests that peptide-loaded chitosan microparticles into guar-gum oral films might be a promising carrier for enhancement of the buccal and intestinal absorption of a relaxing peptide.Patrícia BatistaPedro M. CastroAna Raquel MadureiraBruno SarmentoManuela PintadoMDPI AGarticlebioactive peptidesoral delivery systemchitosanoral filmsTechnologyTEngineering (General). Civil engineering (General)TA1-2040Biology (General)QH301-705.5PhysicsQC1-999ChemistryQD1-999ENApplied Sciences, Vol 11, Iss 9849, p 9849 (2021)
institution DOAJ
collection DOAJ
language EN
topic bioactive peptides
oral delivery system
chitosan
oral films
Technology
T
Engineering (General). Civil engineering (General)
TA1-2040
Biology (General)
QH301-705.5
Physics
QC1-999
Chemistry
QD1-999
spellingShingle bioactive peptides
oral delivery system
chitosan
oral films
Technology
T
Engineering (General). Civil engineering (General)
TA1-2040
Biology (General)
QH301-705.5
Physics
QC1-999
Chemistry
QD1-999
Patrícia Batista
Pedro M. Castro
Ana Raquel Madureira
Bruno Sarmento
Manuela Pintado
Preparation, Characterization and Evaluation of Guar Films Impregnated with Relaxing Peptide Loaded into Chitosan Microparticles
description Background: Biological molecules such as therapeutic proteins and peptides have provided ample opportunities for further improvements in health and wellbeing. However, such biomacromolecules face stability challenges regarding premature processing and digestion, whenever any enteric delivery route is considered. Hence, oral guar films entrapping peptide-containing chitosan microparticles have been developed as a new delivery system to carry and protect therapeutic relaxing peptides. Results: The composite films were characterized regarding physicochemical properties using FTIR as well as peptide encapsulation efficiency, cytotoxicity, and peptide permeability through buccal and intestinal cell-based models. The composite films with 0.18% (<i>w/w</i>) of peptide demonstrated ca. 0.63% of peptide loading efficiency into the chitosan microparticles and to be safe for buccal and intestinal epithelial cells up to 24 h of contact. The permeability assays through TR146 cells to mimic buccal mucosa epithelium and Caco-2/HT29-MTX to mimic duodenum conditions showed that the incorporation of peptide chitosan microparticles into guar-gum oral films offered a faster permeability, when compared with the free peptide and peptide-chitosan-microparticles-loaded chitosan. Conclusion: This study suggests that peptide-loaded chitosan microparticles into guar-gum oral films might be a promising carrier for enhancement of the buccal and intestinal absorption of a relaxing peptide.
format article
author Patrícia Batista
Pedro M. Castro
Ana Raquel Madureira
Bruno Sarmento
Manuela Pintado
author_facet Patrícia Batista
Pedro M. Castro
Ana Raquel Madureira
Bruno Sarmento
Manuela Pintado
author_sort Patrícia Batista
title Preparation, Characterization and Evaluation of Guar Films Impregnated with Relaxing Peptide Loaded into Chitosan Microparticles
title_short Preparation, Characterization and Evaluation of Guar Films Impregnated with Relaxing Peptide Loaded into Chitosan Microparticles
title_full Preparation, Characterization and Evaluation of Guar Films Impregnated with Relaxing Peptide Loaded into Chitosan Microparticles
title_fullStr Preparation, Characterization and Evaluation of Guar Films Impregnated with Relaxing Peptide Loaded into Chitosan Microparticles
title_full_unstemmed Preparation, Characterization and Evaluation of Guar Films Impregnated with Relaxing Peptide Loaded into Chitosan Microparticles
title_sort preparation, characterization and evaluation of guar films impregnated with relaxing peptide loaded into chitosan microparticles
publisher MDPI AG
publishDate 2021
url https://doaj.org/article/d4ce6b091693428d94a20f19796005d4
work_keys_str_mv AT patriciabatista preparationcharacterizationandevaluationofguarfilmsimpregnatedwithrelaxingpeptideloadedintochitosanmicroparticles
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AT anaraquelmadureira preparationcharacterizationandevaluationofguarfilmsimpregnatedwithrelaxingpeptideloadedintochitosanmicroparticles
AT brunosarmento preparationcharacterizationandevaluationofguarfilmsimpregnatedwithrelaxingpeptideloadedintochitosanmicroparticles
AT manuelapintado preparationcharacterizationandevaluationofguarfilmsimpregnatedwithrelaxingpeptideloadedintochitosanmicroparticles
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