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Evaluation of permeation through respiratory epithelium

MucilAir™ and SmallAir™ allow to evaluate intranasal / bronchial / small airways permeation of drugs/xenobiotics

This assay is designed to :

  • Quantify and rank the permeability of compounds
  • Evaluate the efficiency of formulation for inhalation drug delivery

The assay is directional: from apical to basolateral, or from the basolateral to the apical compartment. The test compound is added to the apical or at the basolateral side of MucilAir™. Permeability is measured by monitoring the appearance of the test compound on the other side of the epithelium using LC-MS or ICP-MS.

Mean apparent permeability coefficients (Papp) for the test compound are compared to a reference control with known human absorption rate (Papp).

Permeability constants (Papp A->B) of 33 Reference compounds

Endpoints

Papp, Asymmetry Index, TEER values.

Molecules Papp (cm/s) A→B Papp (cm/s) B→A Asymmetry Ratio
Salicilic Acid 7.7x10⁻⁵ 1.7x10⁻⁵ 0.2
Nicotine 2.1x10⁻⁵ 3.3x10⁻⁵ 1.6
Propanolol.HCl 1.2x10⁻⁵ 1.6x10⁻⁵ 1.3
Ibuprofen 1.1x10⁻⁵ 1.9x10⁻⁵ 1.7
Tripolidine.HCl 9.7x10⁻⁶ 1.2x10⁻⁵ 1.2
Tetracaïne 8.0x10⁻⁶ 1.1x10⁻⁵ 1.3
Dopamine.HCl 3.0x10⁻⁶ 2.5x10⁻⁶ 0.8
Atenolol 2.2x10⁻⁶ 6.7x10⁻⁶ 3.0

Example A->B and B->A transports and corresponding asymmetry ratio

Reference

 
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