Mucus-PVPA (mucus Phospholipid Vesicle-based Permeation Assay): An artificial permeability tool for drug screening and formulation development
2018
Abstract The
mucuslayer covering all mucosal surfaces in our body is the first barrier encountered by drugs before their potential absorption through
epithelial tissues, and could thus affect the drugs’ permeability and their effectiveness. Therefore, it is of key importance to have in vitro permeability models that can mimic this specific environment. For this purpose, the novel
mucusphospholipid vesicle-based permeation assay (
mucus-PVPA) has been developed and used for permeability screening of drugs and formulations. The model proved to be stable under the chosen conditions and demonstrated the ability to discriminate between compounds with different chemical structures and properties. Overall, a decrease in drug permeability was found in the presence of
mucuson top of the PVPA barriers, as expected. Moreover,
mucoadhesive(chitosan-coated) and mucopenetrating (
PEGylated) liposomes were investigated in the newly developed model. The
mucus-PVPA was able to distinguish between the different liposomal formulations, confirming the penetration potential of the tested formulations and the related drug permeability. The
mucus-PVPA model appears to be a promising in vitro tool able to mimic the environment of mucosal tissues, and could therefore be used for further drug permeability screening and formulation development.
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