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. 2023 Nov 29;15(12):2698.
doi: 10.3390/pharmaceutics15122698.

Permeation Protection by Waterproofing Mucosal Membranes

Luisa Coderch  1 , Cristina Alonso  1 , Ana Cristina Calpena  2   3 , Maria Luisa Pérez-García  3   4 , Beatriz Clares-Naveros  5   6 , Anderson Ramos  1 , Meritxell Martí  1
Affiliations

Permeation Protection by Waterproofing Mucosal Membranes

Luisa Coderch et al. Pharmaceutics. .

Abstract

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 to reduce permeation. Transmembrane water loss of different formulations was evaluated, and three of them were selected to be tested on the sublingual mucosa permeation of drugs. Caffeine, ibuprofen, dexamethasone, and ivermectin were applied 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 notable mainly for the low-molecular-weight compounds, decreasing their permeability coefficient by between 40 and 80%. The reinforcement of the barrier function of mucosa provides a reduction or prevention of the permeation of different actives, which could be extrapolated to toxic compounds such as viruses, contaminants, toxins, etc.

Keywords: kinetic permeation; mucosa; permeability; protection.

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Conflict of interest statement

The authors declare no conflict of interest.

Figures

Figure 1
Figure 1
Mean percentage of caffeine (CAF), ibuprofen (IBU), dexamethasone (DEX), and ivermectin (IVE) release applied to the skin (◆), mucosa (⏶), and mucosa modified by formulations F3 (●), F6 (◆), and F16 (■).
Figure 2
Figure 2
Mean percentage of release of caffeine (■), ibuprofen (⏶), dexametasone (●), and ivermectine (◆) applied to the skin, mucosa, and mucosas modified by formulations F3 and F16.
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Grants and funding

This work was supported by the Consejo Superior de Investigaciones Científicas “Modificación de la mucosa como protección frente al SARS-CoV-2” (CSIC-COV19-130).

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