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The Journal of Nuclear Medicine Vol. 39 No. 11 1972-1977
© 1998 by Society of Nuclear Medicine
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Biodistribution and Kinetics of Nasal Carbon-11-Triamcinolone Acetonide

Marc S. Berridge, Donald L. Heald, Gary J. Muswick, Gregory P. Leisure, Ken W. Voelker and Floro Miraldi

Case Western Reserve University/University Hospitals of Cleveland, Division of Radiology, Cleveland, Ohio; Rhône Poulenc Rarer Pharmaceuticals, Inc., Medical Affairs, Collegeville, Pennsylvania

Correspondence: For correspondence or reprints contact: Marc S. Berridge, PhD, Division of Radiology, University Hospitals of Cleveland, 11100 Euclid Ave., Cleveland, OH 44106.

ABSTRACT

PET is a technique with a strong potential for use in drug evaluation and development. In particular, the distribution and pharmacokinetics of locally administered drugs may be advantageously explored noninvasively using labeled compounds. This pilot study was performed to demonstrate the effectiveness of PET for drug development and to determine the human biodistribution and kinetics of triamcinolone acetonide, labeled with 11C, formulated and nasally administered as Nasacort® nasal inhalant. Methods: Carbon-11-labeled triamcinolone acetonide was formulated as the commercial product, and PET scans of the heads of four volunteers were performed in a vertical orientation. Region-of-interest analysis with MRI coregistration was used to analyze the distribution and kinetics in nasal tissues. Results: Deposition of the majority of the dose on target tissues was immediate. Penetration into sinuses was observed. There was moderate redistribution and slow migration of the drug through nasal passages to the throat. Significant amounts of the drug remained in target regions for several hours. Conclusion: PET is an effective means to determine local drug distribution and kinetics.

Key Words: PET • inhaler • nasal • biodistribution • steroid






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Copyright © 1998 by the Society of Nuclear Medicine.