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首页> 外文期刊>Acta biomaterialia >In vitro characterization of a controlled-release ocular insert for delivery of brimonidine tartrate
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In vitro characterization of a controlled-release ocular insert for delivery of brimonidine tartrate

机译：用于释放酒石酸溴莫尼定的控释眼用插入物的体外表征

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摘要

Glaucoma is the second leading cause of blindness in the US. Brimonidine tartrate (BT) is a modern anti-glaucoma agent that is currently administered as frequently as a thrice-daily topical eye drop medication. Accordingly, compliance with BT regimens is low, limiting overall effectiveness. One attempt that has previously proved effective in addressing non-adherence is the formation of ocular inserts, such as the Ocusert?, whose diffusion-based control released an older drug (pilocarpine) for a week-long period. Modern controlled drug-release technology provides an avenue for extending the release of practically any drug (including new drugs such as BT) for as long as 1 month from a singular insert. Currently, no controlled-release formulations for BT exist. This work outlines the development and characterization of a BT-releasing ocular insert designed from poly(lactic co-glycolic) acid/polyethylene glycol (PEG). It was found that a formulation containing 15% PEG can be created that produces a linear BT-release profile corresponding to BT eye drop delivery estimates. Additionally, these inserts were shown, through the use of atomic force microscopy and scanning electron microscopy, to have smooth surfaces and physical properties suitable for ophthalmic use.
机译：青光眼是美国失明的第二大主要原因。酒石酸溴莫尼定（BT）是一种现代抗青光眼药物，目前与每日三次局部滴眼药水一样频繁给药。因此，对BT疗法的依从性低，限制了整体有效性。先前已证明可有效解决不粘连的一种尝试是形成眼部插入物，例如Ocusert ?，其基于扩散的控制释放了一种旧药物（毛果芸香碱）长达一个星期。现代受控药物释放技术为将几乎所有药物（包括BT等新药）从单一插件的释放延长1个月提供了一条途径。当前，不存在用于BT的控释制剂。这项工作概述了由聚（乳酸共乙醇酸）酸/聚乙二醇（PEG）设计的释放BT的眼用插入物的开发和表征。发现可以产生包含15％PEG的制剂，其产生对应于BT滴眼剂递送估计的线性BT释放曲线。另外，通过使用原子力显微镜和扫描电子显微镜，显示了这些插入物具有光滑的表面和适合眼科使用的物理性质。

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