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首页> 外文期刊>Acta biomaterialia >Episcleral drug film for better-targeted ocular drug delivery and controlled release using multilayered poly-epsilon-caprolactone (PCL)
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Episcleral drug film for better-targeted ocular drug delivery and controlled release using multilayered poly-epsilon-caprolactone (PCL)

机译：使用多层聚ε-己内酯（PCL）的硬膜外药物膜可更好地靶向眼内药物递送和控释

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摘要

Triamcinolone acetonide (TA) and poly-epsilon-caprolactone (PCL) were engineered into a micro drug film for episcleral application to better manage chronic vitreoretinal diseases such as proliferative vitreoretinopathy (PVR). Compared to an intravitreal drug injection, this drug film is much safer without breaking into ocular barriers. Compared to a traditional subtenon injection, this drug film demonstrated superior therapeutic duration, better drug bioavailability in the choroid and retina, and better-targeted drug delivery ability. The rabbit eye study demonstrated that using the PCL-TA film led to 5.6 and 3.4 times higher drug AUC in the choroid and the retina respectively than in eyes following a subtenon drug injection. The mean drug residence time in the rabbit choroid was also doubled by using the episcleral TA film (86 days versus 43 days). Remaining TA in the drug film was consistently higher than that in the subtenon space, indicating controlled release of TA by the PCL-TA film. The pharmacokinetics of triamcinolone in the choroid and retina were optimized from typical first-order kinetics to a more sustained release by use of this film. This episcleral film system worked better on rabbit eyes than on guinea pig eyes, indicating that sclera] thickness and eye size may be crucial aspects to consider when choosing an animal model or when designing a transscleral delivery device for human use. This engineered drug film may be very useful in preventing and managing PVR associated with open globe trauma or surgical repair for retinal detachment.
机译：醋酸曲安奈德（TA）和聚ε-己内酯（PCL）被设计成微药物膜，用于巩膜应用，以更好地控制慢性玻璃体视网膜疾病，例如增生性玻璃体视网膜病变（PVR）。与玻璃体内药物注射相比，这种药物膜更安全，且不会闯入眼屏障。与传统的亚腱注射相比，这种药物膜具有更长的治疗时间，在脉络膜和视网膜中更好的药物生物利用度以及更有针对性的药物递送能力。兔眼研究表明，使用PCL-TA膜可以使脉络膜和视网膜中的药物AUC分别比注射亚腱膜药物后的眼睛分别高5.6和3.4倍。通过使用巩膜TA膜，平均药物在兔脉络膜中的停留时间也增加了一倍（86天对43天）。药物膜中残留的TA始终高于亚腱间隙，表明PCL-TA膜可控制TA的释放。通过使用该薄膜，曲安西龙在脉络膜和视网膜中的药代动力学从典型的一级动力学优化为更持久的释放。这种巩膜膜系统在兔眼上比在豚鼠眼上效果更好，表明巩膜的厚度和眼大小可能是选择动物模型或设计供人使用的巩膜递送装置时要考虑的关键方面。这种工程药物膜可能在预防和管理与开放性眼球外伤或视网膜脱离手术修复相关的PVR方面非常有用。

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