Salbutamol

How does it enter smooth muscle cells?

A. Chiappori, C. Folli, A. M. Riccio, E. Caci, D. Descalzi, L. De Ferrari, E. Ingrassia, G. Nicolini, Giorgio Walter Canonica

Research output: Contribution to journalArticle

4 Citations (Scopus)

Abstract

Polyspecific organic cation transporters (OCTs) in human cell membranes are involved in the uptake, distribution and excretion of cationic compounds. Although their relevance to drug disposition in the liver, small intestine and kidney has been investigated previously, less is known about the influence of these transporters on the pharmacokinetics and pharmacodynamics of inhaled drugs. Drugs that are commonly administered by inhalation for the treatment of respiratory diseases, such as glucocorticoids and cationic β 2- agonists, might interact with several of these transporters, which are strongly expressed on the surfaces of airway epithelial cells. We evaluated the expression of OCT3 and measured the in vitro uptake of the short-acting β 2-agonist salbutamol (SALB), alone or in combination with corticosterone (CS) and beclomethasone dipropionate (BDP), by bronchial smooth muscle cells. Our results showed that these cells express the OCT3 transporter and that SALB enters the cell in a transporter-independent fashion. Moreover, CS and BDP have different activities on SALB transport inside the cell. CS increases SALB transport and BDP decreases SALB transport, although neither of these effects are statistically significant. A better understanding of these mechanisms might lead to the improved treatment of airway diseases.

Original languageEnglish
Pages (from-to)541-546
Number of pages6
JournalInternational Journal of Immunopathology and Pharmacology
Volume25
Issue number2
Publication statusPublished - Apr 2012

Fingerprint

Albuterol
Smooth Muscle Myocytes
Beclomethasone
Corticosterone
Pharmaceutical Preparations
Inhalation
Glucocorticoids
Small Intestine
Cations
Pharmacokinetics
Epithelial Cells
Cell Membrane
Kidney
Liver

Keywords

  • β -agonists
  • Bronchial smooth muscle cells
  • Corticosteroids
  • Organic cation transporter

ASJC Scopus subject areas

  • Pharmacology
  • Immunology
  • Immunology and Allergy

Cite this

Chiappori, A., Folli, C., Riccio, A. M., Caci, E., Descalzi, D., De Ferrari, L., ... Canonica, G. W. (2012). Salbutamol: How does it enter smooth muscle cells? International Journal of Immunopathology and Pharmacology, 25(2), 541-546.

Salbutamol : How does it enter smooth muscle cells? / Chiappori, A.; Folli, C.; Riccio, A. M.; Caci, E.; Descalzi, D.; De Ferrari, L.; Ingrassia, E.; Nicolini, G.; Canonica, Giorgio Walter.

In: International Journal of Immunopathology and Pharmacology, Vol. 25, No. 2, 04.2012, p. 541-546.

Research output: Contribution to journalArticle

Chiappori, A, Folli, C, Riccio, AM, Caci, E, Descalzi, D, De Ferrari, L, Ingrassia, E, Nicolini, G & Canonica, GW 2012, 'Salbutamol: How does it enter smooth muscle cells?', International Journal of Immunopathology and Pharmacology, vol. 25, no. 2, pp. 541-546.
Chiappori A, Folli C, Riccio AM, Caci E, Descalzi D, De Ferrari L et al. Salbutamol: How does it enter smooth muscle cells? International Journal of Immunopathology and Pharmacology. 2012 Apr;25(2):541-546.
Chiappori, A. ; Folli, C. ; Riccio, A. M. ; Caci, E. ; Descalzi, D. ; De Ferrari, L. ; Ingrassia, E. ; Nicolini, G. ; Canonica, Giorgio Walter. / Salbutamol : How does it enter smooth muscle cells?. In: International Journal of Immunopathology and Pharmacology. 2012 ; Vol. 25, No. 2. pp. 541-546.
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