Krohne T U, Holz F G, Meyer C H
Universitäts-Augenklinik Bonn, Ernst-Abbe-Str. 2, 53127, Bonn, Deutschland,
Ophthalmologe. 2014 Feb;111(2):113-20. doi: 10.1007/s00347-013-2932-9.
In addition to topical, periocular and systemic administration, intravitreal injection has been established in recent years as an additional standard procedure for ophthalmological drug delivery. This route of administration is now most frequently used for the therapy of retinal diseases with vascular endothelial growth factor (VEGF) inhibitors.
A selective literature review and an analysis of own research data were carried out.
Intravitreal administration achieves high drug concentrations in the target tissue while minimizing systemic drug exposure. Depending on properties such as molecular weight and binding capacity to the neonatal Fc receptor, intravitreally applied VEGF inhibitors can exhibit relevant differences in intraocular and systemic pharmacokinetics. Moreover, the pharmacokinetics can be affected by properties of the individual eye, such as ocular volume, vitreous liquefaction, and prior vitrectomy.
Pharmacokinetics of intravitreally administered drugs determine both the duration of ocular effect and the degree of systemic exposure and are thus of clinical relevance with regard to the reinjection strategy and systemic safety.
除了局部、眼周和全身给药外，玻璃体内注射近年来已成为眼科药物递送的另一种标准方法。目前，这种给药途径最常用于血管内皮生长因子（VEGF）抑制剂治疗视网膜疾病。
进行了选择性文献综述并分析了自身研究数据。
玻璃体内给药可在靶组织中实现高药物浓度，同时将全身药物暴露降至最低。根据分子量和与新生儿Fc受体的结合能力等特性，玻璃体内应用的VEGF抑制剂在眼内和全身药代动力学方面可能存在显著差异。此外，药代动力学可能会受到个体眼睛特性的影响，如眼容积、玻璃体液化和既往玻璃体切除术。
玻璃体内给药药物的药代动力学决定了眼部效应的持续时间和全身暴露程度，因此在再注射策略和全身安全性方面具有临床相关性。
