Abstract
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% (w/w) 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.
Highlights
Oral administration of drug delivery drugs is the most popular route, and different dosage forms have been developed for the oral cavity
Relaxing peptide-loaded chitosan microparticles were prepared by ionic gelation method, and parameters such as particle size, zeta potential, polidispersion index (PDI), association efficiency (AE), and loading capacity were analyzed
An oral delivery system based on the combination guar-gum films and chitosan microparticles was developed, joining the advantages of the orodispersible film with that gained from microcarriers as oral delivery systems for a peptide with relaxing function
Summary
Oral administration of drug delivery drugs is the most popular route, and different dosage forms have been developed for the oral cavity. Several types of colloidal particles have been shown to be capable of encapsulating and improving the bioactivity of proteins Biological molecules such as therapeutic proteins and peptides have provided ample opportunities for further improvements in health and wellbeing. Such biomacromolecules face stability challenges regarding premature processing and digestion, whenever any enteric delivery route is considered. Oral guar films entrapping peptide-containing chitosan microparticles have been developed as a new delivery system to carry and protect therapeutic relaxing peptides. 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
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