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Vol. 28, Issue 2, 205-208, February 2000

Pharmacokinetics of All-trans Retinoic Acid, 13-cis Retinoic Acid, and Fenretinide in Plasma and Brain of Rat

François Le Doze, Daniele Debruyne, Françoise Albessard, Louisa Barre, and Gilles Louis Defer

Laboratory of Pharmacology, Unit of Neurology Dejerine, Unité Propre de Recherche de l'Enseignement Supérieur-Equipe d'accueil 2609.

We have measured the pharmacokinetics of three retinoids, all-trans retinoic acid, 13-cis retinoic acid, and fenretinide in rat blood and rat brain [especially white matter (WM) and gray matter (GM)] to help select retinoids for treating human malignant glioma. All-trans retinoic acid permeated well into the WM, giving peak concentration in WM of 25.7 µg/g, 6 to 7 times higher than the peak serum concentration. There was less 13-cis retinoic acid in WM: area under the curve (AUC)0right-arrow infinity WM/AUC0right-arrow infinity serum = 18.00 µg ml-1 h/32.67 µg ml-1 h. The ratio WM/GM was over 1 for these two compounds, but the half-lives were short in the serum and cerebral tissue (0.57-1.02 h). Fenretinide had different pharmacokinetics: the peak concentrations were in serum (1.7 µg/ml) and WM (1.2 µg/ml)-low, but the AUC0right-arrow infinity was large (25.55 µg ml-1 in serum and 57.53 µg ml-1 in WM) due to its long elimination half-life (13.78 h in serum and 17.77 h in WM). These findings provide information that may be used to select a retinoid and establish therapeutic regimens that provide optimal efficacy with minimal toxicity.

Copyright © 2000 by The American Society for Pharmacology and Experimental Therapeutics


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