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  • Title: Pharmacokinetics of intraocular drug delivery of Oregon green 488-labeled triamcinolone by subtenon injection using ocular fluorophotometry in rabbit eyes.
    Author: Lee SJ, Kim ES, Geroski DH, McCarey BE, Edelhauser HF.
    Journal: Invest Ophthalmol Vis Sci; 2008 Oct; 49(10):4506-14. PubMed ID: 18503001.
    Abstract:
    PURPOSE: To evaluate the transscleral delivery of Oregon Green-labeled triamcinolone acetonide (OGTA) into the eye. METHODS: Ex vivo experiments were performed on rabbit sclera in a Lucite block perfusion chamber. Two hundred microliters OGTA (5 mg/mL) was placed on the outer surface of the sclera for 24 hours. The exposed sclera was divided into two pieces; one half for a washout of OGTA and the other for histology. The concentration of OGTA that diffused through the sclera (n = 6) was measured by fluorometry. Two hundred microliters of OGTA (5 mg/mL) was also injected subtenon into live (n = 6) and euthanatized rabbits (n = 3). Intraocular OGTA concentrations were measured by ocular fluorophotometry. RESULTS: The permeability constant for the transscleral diffusion (K(trans)) of OGTA was 1.12 x 10(-7) +/- 0.08 cm/s (n = 8) during the steady state perfusion. Washout tests showed higher OGTA concentration in the sclera exposed to OGTA for 4 hours than in that exposed for 1 hour. Fluorescent microscopy showed OGTA fluorescence throughout the exposed sclera, as evidence of scleral penetration of OGTA. The maximum OGTA concentration in the retina/choroid after subtenon injection was 25.77 +/- 10.26 ng/mL in the live rabbit at 3 hours and 84.68 +/- 21.04 ng/mL in the euthanatized rabbits at 8 hours. CONCLUSIONS: OGTA is capable of diffusing across isolated rabbit sclera ex vivo and into the retina/choroid via transscleral diffusion from a subtenon depot in vivo. Conjunctival and choroidal circulation decreased the drug delivery of OGTA.
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