preprints.org > chemistry and materials science > medicinal chemistry > doi: 10.20944/preprints202310.1355.v1

Preprint Article Version 1 Preserved in Portico This version is not peer-reviewed

Version 1 : Received: 20 October 2023 / Approved: 20 October 2023 / Online: 23 October 2023 (09:53:37 CEST)

The permeability of the oral or nasal mucosa is higher than that of the skin. Mucosa permeability depends mainly on the thickness and keratinization degree of the tissues. Their permeability barrier is conditioned by the presence of certain lipids. This work has the main aim of reinforcing the barrier effect of oral mucosa with a series of formulations. Sixty-three initial formulations were evaluated for transmembrane water loss, with 16 formulations selected to test on sublingual mucosa. In vitro release tests of caffeine, ibuprofen, dexamethasone and ivermectin were carried out on porcine skin, mucosa and modified mucosa in order to compare the effectiveness of the formulations. A similar permeation profile was obtained in the different membranes: caffeine > ibuprofen ~ dexamethasone > ivermectin. The most efficient formulation was a liposomal formulation composed of lipids that are present in the skin stratum corneum. Impermeability provided by this formulation was really notable mainly for the low molecular weight compounds, decreasing their permeability coefficient between 40-80%. The reinforcement of the barrier function of mucosa provides a reduction or prevention of the permeation of different actives such as viruses, contaminants, toxins, etc.

Mucosa; protection; permeability; kinetic permeation

Chemistry and Materials Science, Medicinal Chemistry

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