Chen Lanlan, Liu Hua, Zhang Qingrong, Huang Houbin
Medical School of Chinese PLA, Beijing, China.
Senior Department of Ophthalmology, The Third Medical Center of Chinese PLA General Hospital, Beijing, China.
Front Pharmacol. 2025 Apr 7;16:1534048. doi: 10.3389/fphar.2025.1534048. eCollection 2025.
The present study aims to evaluate the ocular pharmacokinetics of intravitreal conbercept after retinal scatter laser photocoagulation.
Thirty male Chinchilla rabbits (60 eyes) were used in this study. The control and photocoagulated animals received single bilateral intravitreal injections of conbercept, and the ocular tissues were collected and quantified for drug concentration using ELISA. Statistical analysis was then performed to compare the pharmacokinetic parameters between the control and photocoagulated eyes.
The conbercept concentrations were higher in the control rabbits than the photocoagulated rabbits and reached peak values in all ocular tissues 1 d after intravitreal dosing. The terminal t values in the vitreous humor (4.36 d), aqueous humor (4.19 d), retina (3.94 d), and choroid-RPE (3.84 d) of the control eyes were longer than those in the photocoagulated eyes (3.82 d, 3.69 d, 3.65 d, and 3.58 d, respectively). Conbercept exposure assessed using AUC was lower in the photocoagulated rabbits than control animals in all four ocular matrices ( < 0.01). The clearance and volume of distribution were greater in the photocoagulated eyes than the control eyes, while the mean residence times were shorter in all four matrices.
Retinal scatter laser photocoagulation shortly before single intravitreal injection of conbercept enabled higher drug clearance and shorter half-life values, resulting in lower exposure in the ocular tissues compared to non-photocoagulated conditions. The distinct ocular pharmacokinetics of intravitreal conbercept observed in a rabbit model through retinal scatter laser photocoagulation is expected to enlighten further studies on investigating the optimal order of the combination of photocoagulation and anti-VEGF agents.
本研究旨在评估视网膜散射激光光凝术后玻璃体内注射康柏西普的眼内药代动力学。
本研究使用了30只雄性龙猫兔（60只眼）。对照组和光凝组动物均接受双侧单次玻璃体内注射康柏西普，收集眼组织并使用酶联免疫吸附测定法对药物浓度进行定量。然后进行统计分析以比较对照组和光凝组眼之间的药代动力学参数。
对照组兔眼中康柏西普浓度高于光凝组兔眼，玻璃体内给药后1天在所有眼组织中均达到峰值。对照组眼玻璃体液（4.36天）、房水（4.19天）、视网膜（3.94天）和脉络膜 - 视网膜色素上皮（3.84天）的终末t值长于光凝组眼（分别为3.82天、3.69天、3.65天和3.58天）。在所有四种眼内基质中，用光凝组兔的曲线下面积评估的康柏西普暴露低于对照组动物（<0.01）。光凝组眼的清除率和分布容积大于对照组眼，而在所有四种基质中的平均驻留时间较短。
在单次玻璃体内注射康柏西普前不久进行视网膜散射激光光凝可实现更高的药物清除率和更短的半衰期值，与未光凝的情况相比，导致眼组织中的暴露更低。通过视网膜散射激光光凝在兔模型中观察到的玻璃体内康柏西普独特的眼内药代动力学有望为进一步研究光凝和抗VEGF药物联合使用的最佳顺序提供启示。
