Abstract

In this study, brimonidine tartrate (BRT) based vitamin E tocopheryl polyethylene glycol succinate (TPGS) nanoparticles loaded in situ gel was developed with aim for improvement of drug ocular retention time. Nanoparticle formulation (PS-1) comprising of PLGA (0.1%w/v) and vitamin E TPGS (0.4%w/v) was characterized. It was revealed that formulation exhibited 123.70 ± 0.12 nm, 0.356 ± 0.02, 82.20 ± 2.32% and − 9.85 ± 0.08 mV of mean particle size, polydispersibility index (PDI), percentage entrapment efficiency (% EE) and zeta potential, respectively. Furthermore, optimized nanoparticles (PS-1) were incorporated into poloxamer 407 based in situ system. Formulation upon in vivo ocular tolerability tests were found to be well tolerated. Results showed that nanoparticles loaded in situ gel exhibited sustained and high residence time compared to marketed formulation in animals. Radio-imaging studies demonstrated that radiolabeled nanoparticles loaded in situ gel was effectively retained on corneal surface for longer duration.

抽象的

在这项研究中，开发了基于酒石酸溴莫尼定（BRT）的维生素E生育酚基聚乙二醇琥珀酸酯（TPGS）纳米粒子，该纳米粒子负载在原位凝胶中，旨在改善药物的眼部保留时间。对包含PLGA（0.1％w / v）和维生素E TPGS（0.4％w / v）的纳米颗粒制剂（PS-1）进行了表征。结果表明，该制剂分别显示出123.70±0.12 nm，0.356±0.02、82.20±2.32％和-9.85±0.08 mV的平均粒径，多分散性指数（PDI），截留效率百分比（％EE）和ζ电位。此外，将优化的纳米颗粒（PS-1）并入基于泊洛沙姆407的原位系统中。体内配方眼耐受性测试被发现具有良好的耐受性。结果表明，与在动物市场上出售的制剂相比，负载在原位凝胶中的纳米颗粒表现出持续且高的停留时间。放射成像研究表明，在原位凝胶中加载的放射性标记纳米颗粒可有效保留在角膜表面更长的时间。