Transport of deslorelin, an LHRH agonist, is vectorial and exhibits regional variation in excised bovine nasal tissue

The Journal of Pharmacy and Pharmacology
Kavitha Koushik, U B Kompella

Abstract

The nasal route is a non-invasive alternative route for the delivery of a number of macromolecules, including peptides, proteins and vaccines. The purpose of this study was to determine the regional variation in excised bovine nasal tissue permeability to deslorelin, a nonapeptide luteinizing hormone releasing hormone (LHRH) agonist, and to further elucidate its mechanisms of transport. To this end, this study determined the permeability of deslorelin across different regions of freshly excised bovine nasal mucosa, including the medium turbinate anterior (MTA), medium turbinate posterior (MTP) and the inferior turbinate posterior (ITP) regions. At 37 degrees C, mucoal-to-serosal (m-s) transport of deslorelin across excised bovine nasal mucosa exhibited regional variation, with the % cumulative transport in 6 h being in the order: MTA (0.2 +/- 0.06%) < MTP (1.6 +/- 0.1%) < ITP (2.85 +/- 0.3%). In addition, at 37 degrees C, deslorelin transport across all these nasal regions was vectorial and the mucosal-to-serosal:serosal-to-mucosal (m-s:s-m) transport ratios across MTA, MTP and ITP regions were 1.5, 5.4 and 3.7, respectively. At low temperature (4 degrees C) and at 37 degrees C in the presence of 2,4-dinitrophenol, an energy de...Continue Reading

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Citations

Jul 18, 2009·FASEB Journal : Official Publication of the Federation of American Societies for Experimental Biology·Sneha SundaramUday B Kompella
Nov 19, 2009·Clinical Cancer Research : an Official Journal of the American Association for Cancer Research·Sneha SundaramUday B Kompella
Jan 6, 2006·The Journal of Pharmacy and Pharmacology·Aliasgar Shahiwala, Ambikanandan Misra
Sep 26, 2007·Molecular Pharmaceutics·Nagendra V Chemuturi, Maureen D Donovan

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