Permeation Protection by Waterproofing Mucosal Membranes

Area of Science:

• Biomaterials Science
• Pharmaceutical Sciences
• Dermal and Mucosal Drug Delivery

Background:

• Oral and nasal mucosa exhibit higher permeability than skin due to differences in tissue thickness and keratinization.
• Lipids play a crucial role in the permeability barrier function of mucosal tissues.
• Developing strategies to reinforce mucosal barrier properties is essential for controlled permeation.

Purpose of the Study:

• To create and evaluate formulations designed to strengthen the oral mucosa's barrier effect and reduce permeation.
• To assess the efficacy of selected formulations in reducing the permeation of model drugs across sublingual mucosa.
• To compare the barrier enhancement provided by formulations on different biological membranes.

Main Methods:

• Evaluation of transmembrane water loss for various formulations.
• Testing three selected formulations on sublingual mucosa for drug permeation (caffeine, ibuprofen, dexamethasone, ivermectin).
• Comparative permeation studies using porcine skin, native mucosa, and formulation-modified mucosa.

Main Results:

• A consistent permeation profile across membranes was observed: caffeine > ibuprofen~dexamethasone > ivermectin.
• A liposomal formulation, incorporating lipids found in the skin's stratum corneum, proved most effective.
• This formulation notably reduced the permeability coefficient of low-molecular-weight compounds by 40-80%.

Conclusions:

• Reinforcing the mucosal barrier function effectively reduces or prevents the permeation of active compounds.
• The developed liposomal formulation demonstrates significant potential for enhancing mucosal impermeability.
• This approach could be extended to mitigate the permeation of undesirable substances like viruses, contaminants, and toxins.