The study aimed to evaluate the intraocular pharmacokinetics and efficacy of aflibercept after subconjunctival injection in animal models for treating choroidal neovascularization (CNV) associated with Age-Related Macular Degeneration (AMD). New Zealand albino rabbits received aflibercept (2000 μg/50 μl) in one eye, and the other eye was used as control. At 7, 14, 21 and 28 days, the animals were sacrificed to dissect the ocular tissues, and serum was collected at 1hr, 3 h, 1, 7, 14, 21 and 28 days. The concentration of aflibercept in various ocular tissues and serum were measured using the immunoassay technique. The concentration maximum (C_max) at the Retinal Pigment Epithelium (RPE)-choroid complex and retina in treated eyes was 261.55 and 33.83 ng/gm, respectively. The area under the curve (AUC_0-last) for RPE-Choroid and retina were 2094.02 and 290.33 days. ng/gm respectively. The time maximum (T_max) for the ocular tissues was reached on day 7. In the vitreous humour, a lower level of aflibercept was retrieved. The C_max (1766.84 ng/mL) in the serum was reached on day 1, followed by a decline in the concentration till the end of the study period. In treated eyes, the levels of aflibercept in most of the ocular tissues were maintained for at least 21 days above the invitro IC₅₀ concentration. The results of the efficacy study show that subconjunctival aflibercept could reach the therapeutic target to inhibit CNV. The subconjunctival aflibercept could be a less invasive route for treating CNV with AMD.

该研究旨在评估结膜下注射后在动物模型中治疗与年龄相关性黄斑变性（AMD）相关的脉络膜新生血管（CNV）的眼内药代动力学和阿柏西普的功效。新西兰白化病兔子的一只眼接受了aflibercept（2000μg/ 50μl），另一只眼用作对照。在第7、14、21和28天，处死动物以解剖眼组织，并在1小时，3小时，1、7、14、21和28天收集血清。使用免疫测定技术测量各种眼组织和血清中阿柏西普的浓度。视网膜色素上皮（RPE）-脉络膜复合体和视网膜中的_最高浓度（C _max）分别为261.55和33.83 ng / gm。曲线下面积（AUCRPE的脉络膜和视网膜的_0-last分别为2094.02和290.33天。ng / gm。在第7天达到了眼部组织的_最大时间（T _max）。在玻璃体液中，发现了较低水平的阿柏西普。在第1天，血清中的C _max（1766.84 ng / mL）达到峰值，随后浓度下降直至研究期结束。在接受治疗的眼睛中，大多数眼组织中的阿柏西普水平在高于体外IC ₅₀浓度的条件下至少维持21天。功效研究结果表明，结膜下阿柏西普可以达到抑制CNV的治疗目标。结膜下阿柏西普可能是用AMD治疗CNV的侵入性较小的途径。