糖尿病视网膜病变（DR）是糖尿病常见的致盲性微血管并发症，其发生发展与血管内皮生长因子（VEGF）过度表达密切相关。玻璃体腔注射抗VEGF药物已成为DR，尤其是糖尿病黄斑水肿（DME）和增殖性糖尿病视网膜病变（PDR）的主要治疗方式，而药物眼内药动学特征直接影响治疗方案优化、临床疗效以及用药安全性。系统梳理雷珠单抗、贝伐珠单抗、阿柏西普、康柏西普、法瑞西单抗、哌加他尼的分子特征与药动学规律，分层归纳人体临床、动物实验及模型研究证据。现有研究表明，各类药物在眼内滞留时长、清除速率及全身暴露方面表现出不同特征，但药物半衰期受物种、取样基质、参数估算方法影响，不同研究结果不宜简单横向对比。DR相关玻璃体结构异常，可改变药物扩散和组织转运；玻璃体切除可能加速部分抗VEGF药物的眼内清除，缩短局部滞留及VEGF抑制时间；血-视网膜屏障（BRB）损伤可能增加视网膜通透性并改变后路转运。DR病理状态及眼内结构改变可能增加抗VEGF药物眼内暴露的个体差异，且目前针对DR特异性人体眼内药动学证据仍有限。临床应结合疾病分期、玻璃体状态及既往眼部干预史，优化药物选择与给药间隔，为个体化治疗提供参考。

Diabetic retinopathy (DR) is a common vision-threatening microvascular complication of diabetes mellitus, and its development is closely associated with the overexpression of vascular endothelial growth factor (VEGF). Intravitreal anti-VEGF therapy has become a major treatment strategy for DR, particularly diabetic macular edema (DME) and proliferative diabetic retinopathy (PDR). The intraocular pharmacokinetic properties of these agents directly affect treatment optimization as well as efficacy and safety evaluation. This review summarizes the molecular and pharmacokinetic characteristics of ranibizumab, bevacizumab, aflibercept, conbercept, faricimab, and pegaptanib, while distinguishing among evidence derived from human clinical studies, animal experiments, and model-based estimates. Current evidence indicates that anti-VEGF agents differ in intraocular residence, clearance, and systemic exposure. Because half-life estimates vary with species, sampling matrix, and estimation methods, direct cross-study comparisons should be interpreted cautiously. DR-related vitreous alterations may affect drug diffusion and tissue distribution, while vitrectomy may accelerate intraocular clearance and shorten both drug residence and VEGF suppression. Blood-retinal barrier (BRB) dysfunction may further increase retinal permeability and alter posterior drug transport and clearance. Overall, DR-related ocular changes may contribute to variability in intraocular drug exposure, whereas DR-specific human pharmacokinetic data remain limited. Disease stage, vitreous status, and prior ocular interventions should therefore be considered when optimizing drug selection and dosing intervals.

R969.1