Rubsamen P E, Davis P A, Hernandez E, O'Grady G E, Cousins S W
Department of Ophthalmology, Bascom Palmer Eye Institute, School of Medicine, University of Miami, FL.
Arch Ophthalmol. 1994 Mar;112(3):407-13. doi: 10.1001/archopht.1994.01090150137036.
To test the efficacy of a biodegradable device for the intravitreal sustained release of fluorouracil in the treatment of tractional retinal detachment due to proliferative vitreoretinopathy.
A 6 x 0.9-mm (20-gauge) cylindrical solid implant molded from copolymers of lactide and glycolide admixed with 1 mg of fluorouracil was placed in the vitreous cavity of rabbits in which retinal detachment with proliferative vitreoretinopathy had been initiated. Comparisons of the control (drug-free polymer) and experimental (fluorouracil polymer) groups were made with weekly indirect ophthalmoscopic examinations. In another experiment, the intravitreal concentration of fluorouracil was tested at each time point.
Retinas of eight (89%) of nine rabbits that received the polymer with fluorouracil remained attached compared with only one animal (11%) that received the control polymer without the drug. The therapeutic effect of the drug-containing implant was associated with sustained intravitreal concentrations of fluorouracil between 1 and 13 mg/L for at least 14 days, and fluorouracil concentrations remained above 0.3 microgram/mL for almost 21 days. No evidence of the toxic effects of the drug or polymer implant was observed with electroretinographic and histopathologic study.
Intravitreal implantation of biodegradable polymers containing fluorouracil can prevent proliferation of epiretinal membranes resulting in complicated retinal detachment in an animal model of proliferative vitreoretinopathy and indicate their possible usefulness for intravitreal delivery of therapeutic agents.
测试一种可生物降解装置在玻璃体内持续释放氟尿嘧啶治疗增殖性玻璃体视网膜病变所致牵引性视网膜脱离的疗效。
将由丙交酯和乙交酯共聚物与1毫克氟尿嘧啶混合模制而成的6×0.9毫米（20号）圆柱形固体植入物置于已引发增殖性玻璃体视网膜病变性视网膜脱离的兔玻璃体腔中。通过每周间接检眼镜检查对对照组（不含药物的聚合物）和实验组（含氟尿嘧啶聚合物）进行比较。在另一项实验中，对每个时间点的玻璃体内氟尿嘧啶浓度进行检测。
接受含氟尿嘧啶聚合物的9只兔中有8只（89%）视网膜保持附着，而接受不含药物的对照聚合物的兔只有1只（11%）视网膜保持附着。含药植入物的治疗效果与玻璃体内氟尿嘧啶浓度在1至13毫克/升之间持续至少14天有关，且氟尿嘧啶浓度在近21天内保持高于0.3微克/毫升。视网膜电图和组织病理学研究未观察到药物或聚合物植入物有毒性作用的证据。
在增殖性玻璃体视网膜病变动物模型中，玻璃体内植入含氟尿嘧啶的可生物降解聚合物可防止视网膜前膜增殖导致复杂性视网膜脱离，并表明其在玻璃体内递送治疗药物方面可能有用。
