Mucoadhesive Electrospun Nanofiber-Based Hybrid System with Controlled and Unidirectional Release of Desmopressin

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The sublingual mucosa is an attractive route for drug delivery, although challenged by a continuous flow of saliva that leads to a loss of drug by swallowing. It is of great benefit that drugs absorbed across the sublingual mucosa avoid exposure to the harsh environment of the gastro-in-testinal lumen; this is especially beneficial for drugs of low physicochemical stability such as therapeutic peptides. In this study, a two-layered hybrid drug delivery system was developed for the sublingual delivery of the therapeutic peptide desmopressin. It consisted of peptide-loaded muco-adhesive electrospun chitosan/polyethylene oxide-based nanofibers (mean diameter of 183 ± 20 nm) and a saliva-repelling backing film to promote unidirectional release towards the mucosa. Desmo-pressin was released from the nanofiber-based hybrid system (approximately 80% of the loaded peptide was released within 45 min) in a unidirectional manner in vitro. Importantly, the nanofiber– film hybrid system protected the peptide from wash-out, as demonstrated in an ex vivo flow retention model with porcine sublingual mucosal tissue. Approximately 90% of the loaded desmopressin was retained at the surface of the ex vivo porcine sublingual mucosa after 15 min of exposure to flow rates representing salivary flow.

Original languageEnglish
Article number1458
JournalInternational Journal of Molecular Sciences
Issue number3
Number of pages9
Publication statusPublished - 2022

Bibliographical note

Funding Information:
Funding: This research was funded by The Danish Council for Independent Research, Technology and Production, grant number DFF-6111-00333; the Novo Nordisk Foundation Grand Challenge Program, NNF16OC0021948; and Innovation Fund Denmark PROBIO, project-7076-00053B.

Publisher Copyright:
© 2022 by the authors. Licensee MDPI, Basel, Switzerland.

    Research areas

  • Biopharmaceuticals, Electrospinning, Ex vivo flow retention model, Muco-adhesion, Peptide drug delivery, Sublingual delivery

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