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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2021
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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) |
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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 |
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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 AT pedromcastro preparationcharacterizationandevaluationofguarfilmsimpregnatedwithrelaxingpeptideloadedintochitosanmicroparticles AT anaraquelmadureira preparationcharacterizationandevaluationofguarfilmsimpregnatedwithrelaxingpeptideloadedintochitosanmicroparticles AT brunosarmento preparationcharacterizationandevaluationofguarfilmsimpregnatedwithrelaxingpeptideloadedintochitosanmicroparticles AT manuelapintado preparationcharacterizationandevaluationofguarfilmsimpregnatedwithrelaxingpeptideloadedintochitosanmicroparticles |
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1718437930696966144 |