An intravitreal sustained-release triamcinolone and 5-fluorouracil codrug in the treatment of experimental proliferative vitreoretinopathy
An intravitreal sustained-release triamcinolone and 5-fluorouracil codrug in the treatment of experimental proliferative vitreoretinopathy
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DOI：
10.1001/archopht.116.1.69
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发表时间：
1998-01-01
影响因子：
--
通讯作者：
Jaffe, GJ
中科院分区：
文献类型：
--
作者：
Yang, CS;Khawly, JA;Jaffe, GJ
目的：目的：研究曲安奈德缓释剂（TA）与5-氟尿嘧啶（5-FU）联合用药治疗实验性增生性玻璃体视网膜病变（PVR）的疗效及药代动力学。在不同时间点测定玻璃体腔内曲安奈德和5-氟尿嘧啶的浓度，并进行体外释药试验。通过视网膜电图、临床检查和光学显微镜观察评价毒性反应。结果：用复方药物治疗的眼，PVR分级的严重程度和中度或重度牵拉性脱离的眼的百分比均显著降低。玻璃体内联合药物的治疗效果被持续的玻璃体内曲安奈德和5-氟尿嘧啶水平所抵消。有没有明显的临床或组织病理学检查的眼睛含有TA/S-FU codrug.Conclusions：玻璃体内缓释TAI 5-FU codrug. The药物相关的毒性作用有效地抑制PVR的进展，在兔模型，非常类似于PVR在人类。TA/5-FU联合药物可以同时靶向伤口愈合反应的不同组分。
Objective: To determine the efficacy and pharmacokinetics of an intravitreal sustained-release triamcinolone acetonide and 5-fluorouracil (TA/5-FU) codrug in the treatment of experimental proliferative vitreoretinopathy (PVR).Methods: The therapeutic efficacy of the TA/5-FU codrug was determined in a rabbit model that simulates human PVR. Intravitreal levels of triamcinolone and 5-fluorouracil were measured at different time points and drug release in vitro was tested. Toxic effects were evaluated by electroretinograpy, clinical examination, and light microscopy.Results: Both the severity of PVR grade and the percentage of eyes with moderate or worse tractional detachment were significantly less in eyes treated with the codrug. The therapeutic effect of the intravitreal codrug was paralleled by sustained intravitreal levels of triamcinolone and 5-fluorouracil. There were no drug related toxic effects evident on clinical or histopathologic examination of eyes containing the TA/S-FU codrug.Conclusions: The intravitreal sustained-release TAI 5-FU codrug effectively inhibits the progression of PVR in a rabbit model that closely resembles PVR in humans. The TA/5-FU codrug may simultaneously target different components of the wound-healing response.