Brimonidine tartrate (BRT) is a water-soluble anti-glaucoma drug that is available in ophthalmic solution (Alphagan Z^®). Various ocular barriers prevent permeation and precorneal retention of the drugs within the corneal region. In this study, BRT encapsulated vitamin E-tocopheryl polyethylene glycol succinate (TPGS)-polycaprolactone (PCL) nanoparticles were prepared to improve permeation through different physiological barriers of eyes. Optimized formulation comprising of PCL (0.4% w/v) and vitamin E TPGS (0.5% w/v) was characterized. It was revealed that formulation exhibited 243.40 ± 5.21 nm, 0.103 ± 0.020, 78.87 ± 5.32% and +3.23 ± 0.01 mV of mean particle size, polydispersibility index (PDI), percentage entrapment efficiency (%EE), and zeta potential respectively. Furthermore, optimized BRT loaded nanoparticles were incorporated into a poloxamer based in situ system and was characterized. In vitro study confirmed that around 93.91 ± 3.12% was the highest recorded of cumulative drug release in simulated aqueous humor over 24 h. Optimized formulation upon in vivo ocular irritability and tolerability tests were found to be well tolerated with no signs of irritation. A significant difference in percentage of intraocular pressure (IOP) reduction between marketed eye drop and optimized nanoparticles based in situ gel was observed in the glaucoma induced rabbit model. These experimental data revealed that nanoparticles based thermosensitive in situ gel could be utilized to enhance corneal residence time and ensure consistent IOP reduction.

酒石酸溴莫尼定（BRT）是一种水溶性的抗青光眼药物是在眼用溶液（阿法根ž可用^®）。各种眼屏障可防止药物在角膜区域内渗透和保留在角膜前。在这项研究中，制备了BRT封装的维生素E-生育酚聚乙二醇琥珀酸酯（TPGS）-聚己内酯（PCL）纳米颗粒，以改善通过不同生理屏障的渗透。表征了由PCL（0.4％w / v）和维生素E TPGS（0.5％w / v）组成的优化配方。结果表明，该制剂分别显示出243.40±5.21 nm，0.103±0.020、78.87±5.32％和+3.23±0.01 mV的平均粒径，多分散指数（PDI），包封率（％EE）和Zeta电位。此外，将优化的负载BRT的纳米颗粒掺入基于泊洛沙姆的原位系统中并进行了表征。体外研究证实约为93.91±3。12％是模拟房水在24小时内累积药物释放的最高记录。发现对体内眼刺激性和耐受性测试的优化配方具有良好的耐受性，没有刺激的迹象。在青光眼诱发的兔模型中，观察到市售的眼药水和基于纳米粒子的优化原位凝胶之间的眼内压降低百分比存在显着差异。这些实验数据表明，基于纳米颗粒的热敏原位凝胶可用于延长角膜停留时间并确保持续降低IOP。在青光眼诱发的兔模型中，观察到市售的眼药水和基于纳米粒子的优化原位凝胶之间的眼内压降低百分比存在显着差异。这些实验数据表明，基于纳米颗粒的热敏原位凝胶可用于延长角膜停留时间并确保持续降低IOP。在青光眼诱发的兔模型中，观察到市售的眼药水和基于纳米颗粒的优化原位凝胶之间眼内压降低的百分比存在显着差异。这些实验数据表明，基于纳米颗粒的热敏原位凝胶可用于延长角膜停留时间并确保持续降低IOP。