贝伐单抗经眼部局部和玻璃体内给药后的药代动力学。
Pharmacokinetics of bevacizumab after topical and intravitreal administration in human eyes.
机构信息
Department of Ophthalmology, Tel-Aviv Sourasky Medical Center, Affiliated to the Sackler School of Medicine, Tel Aviv University, Tel Aviv, 6 Weizman Street, Tel-Aviv, 64239, Israel,
出版信息
Graefes Arch Clin Exp Ophthalmol. 2014 Feb;252(2):331-7. doi: 10.1007/s00417-013-2495-0. Epub 2013 Oct 31.
BACKGROUND
Topical bevacizumab is a potential treatment modality for corneal neovascularization, and several recent studies have demonstrated its efficacy. No previous study of the pharmacokinetics of topical bevacizumab has been performed in human eyes. The purpose of this study is to investigate the pharmacokinetics of topical administration of bevacizumab in human eyes, and also to compare the pharmacokinetics of intravitreal bevacizumab injections with previously reported data.
METHODS
Twenty-two (22 eyes) were included in this study, and divided into four groups: eight patients received topical bevacizumab and aqueous samples were obtained 1 hour later during cataract extraction surgery (group 1), eight patients received topical bevacizumab and vitreous samples were obtained 1 day later during pars-plana vitrectomy (PPV) (group 2), three patients received intravitreal bevacizumab and vitreous samples were obtained during PPV (group 3). Vitreous samples from three patients who received no bevacizumab served as controls (group 4). All samples underwent enzyme-linked immunosorbent assay to detect bevacizumab.
RESULTS
No bevacizumab was detected in the aqueous or vitreous of any topically treated eyes. The mean vitreal half-life for intravitreally injected bevacizumab was 4.9 days in four non-vitrectomized eyes and 0.66 days in one previously vitrectomized eye.
CONCLUSIONS
Topically administered bevacizumab does not penetrate the cornea into the anterior chamber and vitreous cavity, indicating that topical use for treating corneal neovascularization has minimal risk of intraocular penetration and adverse events related to intraocular vascular endothelial growth factor inhibition. The half-life following intravitreal bevacizumab injection measured in this study is comparable to that of previous reports, and includes the first demonstration of a significantly reduced half-life following intravitreal injection in a previously vitrectomized eye.
背景
局部贝伐单抗是治疗角膜新生血管的一种潜在治疗方法，多项近期研究已证实其疗效。目前尚无研究探讨局部贝伐单抗在人眼内的药代动力学。本研究旨在研究局部应用贝伐单抗在人眼内的药代动力学，并与之前报道的数据比较玻璃体内注射贝伐单抗的药代动力学。
方法
本研究共纳入 22 只眼（22 只眼），分为 4 组：8 例患者于白内障摘除术时局部滴注贝伐单抗并于 1 小时后采集房水样本（组 1），8 例患者于玻璃体切割术（PPV）时局部滴注贝伐单抗并于 1 天后采集玻璃体样本（组 2），3 例患者接受玻璃体内注射贝伐单抗并于 PPV 时采集玻璃体样本（组 3）。3 例未接受贝伐单抗治疗的患者的玻璃体样本作为对照组（组 4）。所有样本均采用酶联免疫吸附试验检测贝伐单抗。
结果
未在任何局部用药眼的房水或玻璃体内检测到贝伐单抗。4 只未行玻璃体切割的眼内玻璃体内注射贝伐单抗的平均半衰期为 4.9 天，1 只先前已行玻璃体切割的眼内半衰期为 0.66 天。
结论
局部应用贝伐单抗不能穿透角膜进入前房和玻璃体腔，表明局部应用治疗角膜新生血管的方法发生眼内穿透和与抑制眼内血管内皮生长因子相关的不良事件的风险极小。本研究中测量的玻璃体内注射贝伐单抗的半衰期与之前的报道相似，并且首次证明在先前已行玻璃体切割的眼中半衰期明显缩短。
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