PMID: 8587046Nov 1, 1995Paper

Improvement of nasal bioavailability of luteinizing hormone-releasing hormone agonist, buserelin, by cyclodextrin derivatives in rats

Journal of Pharmaceutical Sciences
K MatsubaraK Uekama

Abstract

The effects of chemically modified cyclodextrins on the nasal absorption of buserelin, an agonist of luteinizing hormone-releasing hormone, were investigated in anesthetized rats. Of the cyclodextrins tested, dimethyl-beta-cyclodextrin (DM-beta-CyD) was the most effective in improving the rate and extent of the nasal bioavailability of buserelin. Fluorescence spectroscopic studies indicated that the cyclodextrins formed inclusion complexes with buserelin, which may reduce the diffusibility of buserelin across the nasal epithelium and may participate in the protection of the peptide against enzymatic degradation in the nasal mucosa. Additionally, the cyclodextrins increased the permeability of the nasal mucosa, which was the primary determinant based on the multiple regression analysis of the nasal absorption enhancement of buserelin. Scanning electron microscopic observations revealed that DM-beta-CyD induced no remarkable changes in the surface morphology of the nasal mucosa at a minimal concentration necessary to achieve substantial absorption enhancement. The present results suggest that DM-beta-CyD could improve the nasal bioavailability of buserelin and is well-tolerated by the nasal mucosa of the rat.

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Citations

Jun 11, 2005·Pharmaceutical Research·Laïla BoulmedaratElias Fattal
Mar 17, 2004·European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Für Pharmazeutische Verfahrenstechnik E.V·A O KamphorstR D Sinisterra
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Aug 12, 2004·Chemical & Pharmaceutical Bulletin·Kaneto Uekama
Jul 6, 2004·Yakugaku zasshi : Journal of the Pharmaceutical Society of Japan·Hidetoshi Arima
Dec 4, 2004·Yakugaku zasshi : Journal of the Pharmaceutical Society of Japan·Kaneto Uekama
Jan 5, 2012·Yakugaku zasshi : Journal of the Pharmaceutical Society of Japan·Kaneto Uekama
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