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Expression of Concern.
To determine whether adverse effects such as elevated intraocular pressure
and cataracts, which are lower with dexamethasone when compared with
fluocinolone acetonide or triamcinolone acetonide, may be explained in part
by the differences in drug lipophilicity and partitioning of these drugs
into the trabecular meshwork and lens.
The n-octanol/phosphate-buffered saline (pH 7.4) partition coefficient (log
distribution coefficient [D]) and bovine/human ocular tissue partition
coefficients were determined for triamcinolone, prednisolone, dexamethasone,
fluocinolone acetonide, triamcinolone acetonide, and budesonide at
The log D of the corticosteroids ranged from 0.712 to 2.970. The ranges of
tissue:PBS partition coefficients following drug incubation at 0.4, 2.0, and
10.0 μg/mL were 0.35 to 1.56, 0.30 to 2.12, and 0.30 to 1.95,
respectively, for the bovine lens, 0.87 to 4.18, 0.71 to 4.40, and 0.69 to
5.86, respectively, for the human lens, and 2.98 to 9.48, 2.41 to 9.16, and
1.71 to 9.96, respectively, for the bovine trabecular meshwork. In general,
tissue partitioning showed a positive correlation with log D. Dexamethasone,
with lipophilicity less than triamcinolone acetonide and fluocinolone
acetonide, exhibited the least amount of partitioning in the trabecular
meshwork and lens among these 3 corticosteroids commonly used for treating
diseases at the back of the eye.
Binding of corticosteroids to the trabecular meshwork and lens increases as
drug lipophilicity increases.
Less lipophilic corticosteroids with limited partitioning to the trabecular
meshwork and lens may result in reduced incidence of elevated intraocular
pressure and cataracts.