Brain permeability of inhaled corticosteroids

Journal of Pharmacy and Pharmacology

Volumn 57, Issue 9, 2005, Pages 1159-1167

  Arya, Vikram ^a   Issar, Manish ^a   Wang, Yaning ^a   Talton, James D ^b   Hochhaus, Guenther ^a  

^a UNIVERSITY OF FLORIDA HEALTH   (United States)

^b NANO ADM Advanced Development and Manufacturing Center   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

BECLOMETASONE; BECLOMETASONE DIPROPIONATE; BECLOMETASONE MONOPROPIONATE; BRAIN RECEPTOR; BUDESONIDE; CORTICOSTEROID; FLUTICASONE PROPIONATE; GENE PRODUCT; GLYCOPROTEIN P; MULTIDRUG RESISTANCE PROTEIN 1; MULTIDRUG RESISTANCE PROTEIN 1A; TRIAMCINOLONE ACETONIDE; UNCLASSIFIED DRUG;

ANIMAL TISSUE; ARTICLE; BIOASSAY; BRAIN; CONTROLLED STUDY; CORTICOSTEROID THERAPY; DRUG PENETRATION; DRUG RECEPTOR BINDING; DRUG STRUCTURE; INHALATIONAL DRUG ADMINISTRATION; KIDNEY; KNOCKOUT MOUSE; LIPOPHILICITY; LIVER; MOUSE; NONHUMAN; RAT; RECEPTOR BINDING ASSAY; RECEPTOR OCCUPANCY;

ADMINISTRATION, INHALATION; ADRENAL CORTEX HORMONES; ANDROSTADIENES; ANIMALS; BECLOMETHASONE; BRAIN; BUDESONIDE; DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG EVALUATION, PRECLINICAL; INJECTIONS, INTRAVENOUS; INTUBATION, INTRATRACHEAL; KIDNEY; LIVER; MICE; MICE, KNOCKOUT; P-GLYCOPROTEIN; PARTICLE SIZE; PERMEABILITY; POWDERS; PRODRUGS; RATS; RATS, INBRED F344; RECEPTORS, STEROID; SPECIES SPECIFICITY; TIME FACTORS; TRIAMCINOLONE ACETONIDE;

EID: 25844432138     PISSN: 00223573     EISSN: None     Source Type: Journal    
DOI: 10.1211/jpp.57.9.0010     Document Type: Article

References (21)

1. Ballard, P. L., Baxter, J. D., Higgins, S. J., Rousseau, G. G., Tomkins, G. M. (1974) General presence of glucocorticoid receptors in mammalian tissues. Endocrinology 94: 998-1002
2. Buchwald, P., Bodor, N. (2004) Soft glucocorticoid design: structural elements and physicochemical parameters determining receptor-binding affinity. Pharmazie 59: 396-404
3. Christians, U., Jacobsen, W., Benet, L. Z., Lampen, A. (2002) Mechanisms of clinically relevant drug interactions associated with tacrolimus. Clin. Pharmacokinet. 41: 813-851
4. deKloet, E. R. (1997) Why dexamethasone poorly penetrates in brain. Stress 2: 13-20
5. Dilger, K., Schwab, M., Fromm, M. F. (2004) Identification of budesonide and prednisone as substrates of the intestinal drug efflux pump P-glycoprotein. Inflamm. Bowel Dis. 10: 578-583
6. Farrell, R. J., Kelleher, D. (2003) Glucocorticoid resistance in inflammatory bowel disease. J. Endocrinol. 178: 339-346
7. Greiner, B., Eichelbaum, M., Fritz, P., Kreichgauer, P. H., Richter, O. V., Zundler, J., Kroemer, H. K. (1999) The role of intestinal P-glycoprotein in the interaction of digoxin and rifampin. J. Clin. Invest. 104: 147-153
8. Hochhaus, G., Gonzalez Rothi, R. J., Lukyanov, A., Derendorf, H., Schreier, H., Costa, T. D. (1995) Assessment of glucocorticoid lung targeting by ex vivo receptor binding studies in rats. Pharm. Res. 12: 134-137
9. Karssen, A. M., Meijer, O. C., van der Sandt, I. C., Lucassen, P. J., de Lange, E. C., de Boer, A. G., de Kloet, E. R. (2001) Multidrug resistance P-glycoprotein hampers the access of cortisol but not of corticosterone to mouse and human brain. Endocrinology 142: 2686-2694
10. Karssen, A. M., Meijer, O. C., van der Sandt, I. C., De Boer, A. G., De Lange, E. C., De Kloet, E. R. (2002) The role of the efflux transporter P-glycoprotein in brain penetration of prednisolone. J. Endocrinol. 175: 251-260
11. Mayer, U., Wagenaar, E., Beijnen, J. H., Smit, J. J. M., Meijer, O. C., Asperen, J. V., Borst, P., Schinkel, A. H. (1996) Substantial excretion of digoxin via the intestinal mucosa and prevention of long term digoxin accumulation in the brain by mdr1a P-glycoprotein. Br. J. Cancer 119: 1038-1044
12. Medh, R. D., Lay, R. H., Schmidt, T. J. (1998) Agonist-specific modulation of glucocorticoid receptor-mediated transcription by immunosuppressants. Mol. Cell. Endocrinol. 138: 11-23
13. Meijer, O. C., de Lange, E. C., Breimer, D. D., de Boer, A. G., Workel, J. O., de Kloet, E. R. (1998) Penetration of dexamethasone into brain glucocorticoid targets is enhanced in mdr1A P-glycoprotein knockout mice. Endocrinology 139: 1789-1793
14. Schinkel, A. H., Smit, J. J., Telligen, O. V., Beijnen, J. H., Wagenaar, E., van Deemter, L., Mol, C. A., van der Valk, M. A., Robanus-Maandag, E. C., te Riele, H. P., Berns, A. J. M., Borst, P. (1994) Disruption of the mouse mdr1a P-glycoprotein gene leads to a deficiency in the blood brain barrier and to increased sensitivity of drugs. Cell 77: 491-502
15. Schinkel, A. H., Wagenaar, E., van Deemter, L., Mol, C. A., Borst, P. (1995) Absence of mdr 1A p-glycoprotein in mice affects tissue distribution and the pharmacokinetics of dexamethasone, digoxin, and cyclosporin A. J. Clin. Invest. 96: 1698-1705
16. Schinkel, A. H., Wagenaar, E., Mol, C. A., van Deemter, L. (1996) P-Glycoprotein in the blood-brain barrier of mice influences the brain penetration and pharmacological activity of many drugs. J. Clin. Invest. 97: 2517-2524
17. Suarez, S., Gonzalez-Rothi, R. J., Schreier, H., Hochhaus, G. (1998) Effect of dose and release rate on pulmonary targeting of liposomal triamcinolone acetonide phosphate. Pharm. Res. 15: 1461-1465
18. Verschraagen, M., Koks, C. H. W., Schellens, J. H. M., Beijen, J. H. (1999) P-glycoprotein system as a determinant of drug interactions: the case of digoxin-verapamil. Pharmacol. Res. 40: 301-306
19. Wandel, C., Kim, R. B., Guengerich, P., Wood, A. J. J. (2000) Mibefradil is a P-glycoprotein substrate and a potent inhibitor of both P-glycoprotein and CYP 3A in vitro. Drug Metab. Dispos. 28: 895-898
20. Wang, Y., Hochhaus, G. (2002) Pulmonary targeting of beclomethasone dipropionate in rats. AAPS Annual Meeting, Toronto, Canada, November 2002
21. Yates, C. R., Chang, C., Kearbey, J. D., Yasuda, K., Schuetz, E. G., Miller, D. D., Dalton, J. T., Swaan, P. W. (2003) Structural determinants of P-glycoprotein-mediated transport of glucocorticoids. Pharm. Res. 20: 1794-1803