Abstract
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-intestinal 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 mucoadhesive 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. Desmopressin 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.
Highlights
Relevant Doses of Desmopressin Loaded in Nanofiber–Film Hybrid System
A two-layered hybrid drug delivery system, which consisted of a mucoadhesive electrospun chitosan-based nanofiber mat and a saliva-repelling backing film (Figure 1a), was developed
It is important to note that the peptide delivery system is considered biocompatible, as all selected excipients are biocompatible, and the electrospun nanofibers were prepared using a minimum amount of acetic acid (0.7% (w/w))
Summary
Drugs delivered via the oral cavity avoid the harsh environment of the gastro-intestinal tract and bypass the hepatic firstpass metabolism These factors are beneficial for drugs, which are prone to enzymatic degradation and sensitive to the low pH of the stomach [4]. Formulations for sublingual administration can be handled by the patient as the ventral side of the tongue is readily accessible and the quick removal of the formulation is possible if needed. Such formulations can be administered without water, which is beneficial for patient groups with swallowing difficulties—e.g., the elderly or small children [5]
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