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  • An improved primary human nasal cell culture for the simultaneous determination of transepithelial transport and ciliary beat frequency.

An improved primary human nasal cell culture for the simultaneous determination of transepithelial transport and ciliary beat frequency.

The Journal of pharmacy and pharmacology (2009-07-11)
Roel Mallants, Valerie Vlaeminck, Mark Jorissen, Patrick Augustijns
ABSTRACT

The aim was to establish a preclinical in-vitro system of the nasal mucosa for the simultaneous evaluation of nasal absorption and effects on ciliary activity. Human nasal epithelial cells were grown in collagen-coated transport inserts with transparent polyethylene terephthalate membranes (3 mum). Transepithelial transport and ciliary beat frequency values were measured every 15 min for 1 h. The apparent permeability coefficients (P(app)) for atenolol (mainly paracellular transport) and propranolol (transcellular transport) amounted to 0.1 +/- 0.1 and 23.7 +/- 0.6 x 10(-6) cm/s, respectively, illustrating that the system can be used to discriminate between high permeability and low permeability compounds. Transport of talinolol (substrate for the P-glycoprotein efflux carrier) did not reveal polarity (0.3 +/- 0.2 and 0.2 +/- 0.1 x 10(-6) cm/s for absorptive and secretory transport, respectively) and was not affected by verapamil (10 muM), suggesting the absence of P-glycoprotein in the nasal cell culture. No significant effects of atenolol, propranolol and talinolol on ciliary beat frequency were observed (98 +/- 20% of the control condition after 60 min). Chlorocresol significantly decreased the ciliary activity but this decrease was not accompanied by effects on the transepithelial transport of atenolol, propranolol and talinolol. A new system was developed which offers possibilities as a fast screening tool for studying the potential of compounds for nasal drug administration, since permeability and a possible cilio-toxic effect can be assessed simultaneously.

MATERIALS
Product Number
Brand
Product Description

Supelco
4-Chloro-3-methylphenol, analytical standard
Sigma-Aldrich
4-Chloro-3-methylphenol, ≥98.0% (HPLC)
Sigma-Aldrich
4-Chloro-3-methylphenol, 99%