Tear-Driven Phase Transition Microemulsion for Ocular Delivery of Dexamethasone in the Effective Treatment of Uveitis

The goal of this study was to develop dexamethasone-loaded tear-driven phase transition microemulsions (PTMEs) to effectively treat uveitis. PTMEs were prepared using the oil titration method. Physicochemical parameters, <i>in vitro</i> release, and ocular irritation studies were performed. The <i>in vivo</i> study, total cell count, and total protein content were estimated on the rabbit eye model. The study revealed that developed PTMEs had nanoglobule sizes, acceptable physicochemical properties, and prolonged drug release. Ex-vivo and in-vivo studies concluded that higher permeability and improved anti-inflammatory properties were observed for PTMEs compared to marketed formulation. The prepared PTMEs showed a sustained release pattern and enhanced therapeutic effectiveness, making them a promising alternative to conventional eye drops for treating uveitis.

本研究旨在开发负载地塞米松的泪液驱动相变微乳液（tear-driven phase transition microemulsions，PTMEs），用于葡萄膜炎的有效治疗。本研究采用油滴定法制备该PTMEs，并对其理化参数、体外（in vitro）释药特性及眼部刺激性试验展开考察。通过兔眼模型开展体内（in vivo）研究，检测眼部样本的细胞总数与总蛋白含量。研究结果显示，所制备的PTMEs具有纳米级球粒粒径、良好的理化性质，且可实现长效释药。离体（ex vivo）与体内研究均证实，相较于市售制剂，该PTMEs具备更高的眼部渗透性能与更优异的抗炎活性。所制备的PTMEs呈现稳定的缓释模式且治疗效果显著提升，有望成为治疗葡萄膜炎的常规滴眼液的潜在替代方案。