Inhibition of Experimental Intraocular Proliferation with Intravitreous 5-Fluouracil

Kulnig, W; Binder, Susanne; Riss, B.; Skorpik, Christian

doi:10.1159/000309371

Cited by 18 publications

(7 citation statements)

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“…Binder and associates found that 25% of rabbit eyes receiving an intravitreal injection of 1 mg 5FU demonstrated narrowing of the retinal vessels and hemorrhage [2]. Kulnig demonstrated by transmission electron microscopy retinal damage in rabbit eyes following the intravitreal administration of 5FU in a 1-mg dose [13].…”

Section: Discussionmentioning

confidence: 99%

“…Therapeutic intraocular levels of 5FU can be achieved by intravitreal or subconjunctival administration [7]. However, frequent injections are needed to maintain therapeutic levels, and potentially toxic levels can occur immediately following an intravitreal injection of 1 mg into the rabbit eye [13,2]. A method that would increase the ocular penetration of a drug after subconjunctival injection, or slowly release the drug after intravitreal injection to increase its half-life, would be advantageous.…”

Section: Introductionmentioning

confidence: 99%

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Liposome-encapsulated3H-5FU in rabbits

et al. 1989

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We compared the pharmacokinetics of liposome-encapsulated tritiated 5-fluorouracil (3H-5FU-Lipo) to 3H-5FU in buffered saline (3H-5FU-PBS) after subconjunctival or intravitreal injection into rabbit eyes. Liposomes were prepared using phosphatidylcholine, phosphatidic acid, and alpha-tocopherol. Following a unilateral subconjunctival injection of either 3H-5FU-Lipo or 3H-5FU-PBS, rabbits were sacrificed at 0.5, 1, 4, and 8 hours. Significantly higher (p less than 0.05) drug levels were achieved with the encapsulated drug in the vitreous at all four time points and in the aqueous at three of four time points. Following bilateral intravitreal injections of 500 micrograms of 5FU in 0.1 ml, as either 3H-5FU-Lipo or 3H-5FU-PBS injected rabbits were sacrificed at 0, 6, 12, 24, and 48 hours. Vitreal drug levels were significantly higher (p less than 0.05) with encapsulated drug at all time points from 6 hours on. At 48 hours, the vitreal level with the encapsulated drug was 578 +/- 0.23 micrograms/ml compared with 1.06 +/- 0.07 micrograms/ml for 3H-5FU-PBS.

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Section: Discussionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Liposome-encapsulated3H-5FU in rabbits

et al. 1989

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“…fixed and further processed for histologic and electron-microscopic examination [Kulnig et al, 1984).…”

Section: Histology and Electron Microscopymentioning

confidence: 99%

“…Antiproliferative preparations, such as dexamethasone alcohol, triamcinolone acetonide, 5-fluoracil and daunomicin, have proven their effectiveness in experimental conditions [Tano ct al., 1980;Binder, 1982;Blumenkranz et al, 1983: Binder et al, 1983Kulnig et al, 1984]. Their disadvantages, however, have also become manifest, as e.g.…”

Section: Introductionmentioning

confidence: 99%

High-Energy Electrons Used to Inhibit Experimental Intraocular Proliferation and Detachment

Binder

Skorpik²,

Paroussis³

et al. 1987

Ophthalmologica

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Irradiation of rabbit eyes with high-energy electrons was used to test the inhibition of experimental intraocular proliferation and retinal detachment, produced by intravitreal implantation of 250,000 homologous fibroblasts. After irradiation with 2,000 rad, started 5 days after implantation, 45% of eyes (9 of 20) still manifested traction detachment. When the dose was increased to 3,000 rad and radiation treatment was started 1 day after implantation, proliferation and traction detachment were observed in only 10% of eyes (2 of 20). No acute damage to retinal tissue or nerve fibers was observed. Because it is easily available, simple in application and dose adjustment, and without toxic side effects, radiation therapy should be considered as an effective alternative to drug treatment for the inhibition of intraocular proliferation and detachment. Statistically significant results of this investigation suggest its use combined with surgery in certain reproliferative cases in man.

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“…Methylzellulose and Dexamethason Augentropfen erwiesen sich auch als symptomlindernde Therapie der Nebenwirkungen.5FU erwies sich als effektiver Inhibitor von Fibroblastenwachstum [62] and wird aufgrund dieser Eigenschaft auch bei chirurgischen Eingriffen in der Augenheilkunde verwendet. Es wurde sowohl intravitreal als auch subconjunctival an Tiermodellen injiziert um intraokulare Proliferationen zu inhibieren[63][64][65][66][67][68][69]. Seine lokale Gewebswirkung, kurze Halbwertszeit, leichte Administration and leichte Dosierbarkeit machten 5FU auch als Wundheilungshemmer in der Glaukomchirurgie beliebt…”

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