Intravitreal administration is widely used in ophthalmological practice to maintain therapeutic drug levels near the neuroretina and because drug delivery systems are necessary to avoid reinjections and sight-threatening side effects. However, currently there is no intravitreal treatment for glaucoma. The brimonidine-LAPONITE® formulation was created with the aim of treating glaucoma for extended periods with a single intravitreal injection. Glaucoma was induced by producing ocular hypertension in two rat cohorts: [BRI-LAP] and [non-bri], with and without treatment, respectively. Eyes treated with brimonidine-LAPONITE® showed lower ocular pressure levels up to week 8 (p < 0.001), functional neuroprotection explored by scotopic and photopic negative response electroretinography (p = 0.042), and structural protection of the retina, retinal nerve fibre layer and ganglion cell layer (p = 0.038), especially on the superior-inferior axis explored by optical coherence tomography, which was corroborated by a higher retinal ganglion cell count (p = 0.040) using immunohistochemistry (Brn3a antibody) up to the end of the study (week 24). Furthermore, delayed neuroprotection was detected in the contralateral eye. Brimonidine was detected in treated rat eyes for up to 6 months. Brimonidine-LAPONITE® seems to be a potential sustained-delivery intravitreal drug for glaucoma treatment.

中文翻译：

---

在青光眼动物模型的整个随访6个月中，溴莫尼定-LAPONITE®玻璃体内制剂具有降压和神经保护作用

玻璃体内给药在眼科实践中被广泛使用，以维持神经视网膜附近的治疗药物水平，并且因为药物输送系统对于避免再次注射和威胁视力的副作用是必需的。但是，目前尚无玻璃体内治疗青光眼的方法。制备溴莫尼定-LAPONITE®制剂的目的是通过单次玻璃体内注射长期治疗青光眼。在两个大鼠队列中，[BRI-LAP]和[non-bri]分别通过产生和治疗高眼压而诱发青光眼。用溴莫尼定-LAPONITE®处理的眼睛在第8周时表现出较低的眼压水平（p <0.001），通过暗视和视神经阴性视网膜电图检查发现了功能性神经保护（p= 0.042）以及对视网膜，视网膜神经纤维层和神经节细胞层的结构保护（p = 0.038），尤其是在光学相干断层扫描所探讨的上下轴上，这被较高的视网膜神经节细胞计数所证实（p直到研究结束（第24周）之前，使用免疫组织化学（Brn3a抗体）= 0.040）。此外，在对侧眼中检测到延迟的神经保护。在治疗的大鼠眼睛中检测到溴莫尼定长达6个月。溴莫尼定-LAPONITE®似乎是用于青光眼治疗的潜在持续递送玻璃体内药物。