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Nasal drug delivery has attracted significant attention as an alternative route to deliver drugs having poor bioavailability. Large-molecule drugs such as peptides, and central nervous system drugs, would benefit from intranasal delivery. Drug absorption after intranasal application depends on the nasal retention of the drug, which is determined by the nasal mucociliary clearance. Mucociliary clearance (MC) is an important determinant of the rate and extent of nasal drug absorption. The aim of the present study was to clarify the effect of changes in MC on in vivo drug absorption after nasal application, and to justify the pharmacokinetic model to which the MC parameter was introduced, to enable prediction of bioavailability after intranasal administration. The pharmacokinetics of norfloxacin (NFX) after intranasal administration were evaluated following the modification of nasal MC by pretreatment with the MC inhibitors propranolol and atropine and the MC enhancers terbutaline and acetylcholine chloride. From the relationship between nasal MC and bioavailability after nasal application, prediction of drug absorption was attempted based on our pharmacokinetic model. Propranolol and atropine enhanced the bioavailability of NFX by 90% and 40%, respectively, while the bioavailability decreased by 30% following terbutaline and 40% following acetylcholine chloride. As a result of changes in MC function, nasal drug absorption was changed depending on the nasal residence time of the drug. Based on our pharmacokinetic model, the nasal drug absorption can be precisely predicted, even when the MC is changed. This prediction system allows the quantitative evaluation of changes in drug absorption due to changes in nasal MC, and is expected to contribute greatly to the development of nasal formulations.
This article was published in the following journal.
Name: Molecular pharmaceutics
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Porphyrins which are combined with a metal ion. The metal is bound equally to all four nitrogen atoms of the pyrrole rings. They possess characteristic absorption spectra which can be utilized for identification or quantitative estimation of porphyrins and porphyrin-bound compounds.
Uptake of substances through the nasal mucosa.
The qualitative or quantitative estimation of the likelihood of adverse effects that may result from exposure to specified health hazards or from the absence of beneficial influences. (Last, Dictionary of Epidemiology, 1988)
A chronic inflammation in which the NASAL MUCOSA gradually changes from a functional to a non-functional lining without mucociliary clearance. It is often accompanied by degradation of the bony TURBINATES, and the foul-smelling mucus which forms a greenish crust (ozena).
Fluid obtained by irrigation or washout of the nasal cavity and NASAL MUCOSA. The resulting fluid is used in cytologic and immunologic assays of the nasal mucosa such as with the NASAL PROVOCATION TEST in the diagnosis of nasal hypersensitivity.
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