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Permeation Protection by Waterproofing Mucosal Membranes.

Luisa Coderch1, Cristina Alonso1, Ana Cristina Calpena2,3

  • 1Surfactants and Nanobiotechnology Department, Institute of Advanced Chemical of Catalonia of CSIC (IQAC-CSIC), Jordi Girona 18-26, 08034 Barcelona, Spain.

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|December 23, 2023
PubMed
Summary
This summary is machine-generated.

This study developed liposomal formulations to enhance oral mucosa barrier function, significantly reducing drug permeation. These findings offer potential for protecting against various permeants, including toxins.

Keywords:
kinetic permeationmucosapermeabilityprotection

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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.