论文标题：Self-implantable double-layered micro-drug-reservoirs for efficient and controlled ocular drug delivery

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作者：Aung Than, Chenghao Liu, Hao Chang, Phan Khanh Duong, Chui Ming Gemmy Cheung, Chenjie Xu, Xiaomeng Wang, Peng Chen

发表时间：2018/11/06

数字识别码： 10.1038/s41467-018-06981-w

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《自然-通讯》发表的一篇论文Self-implantable double-layered micro-drug-reservoirs for efficient and controlled ocular drug delivery介绍了一种可以将药物递送至眼睛来治疗疾病的微型眼贴。该装置已在小鼠身上进行了测试，有望使患者将来能够在对家中进行眼部疾病治疗。

图1：接触性眼贴用于递送药物。图源：Than等

在治疗威胁视力的疾病（如青光眼和年龄相关性黄斑变性）时，许多药物直接入眼是最安全和最有效的。但是，注射可能引起不适、感染和严重眼损伤等问题，滴眼液则可能会被洗掉并且通常效率低下。

新加坡南洋理工大学的陈鹏及其同事开发了一种毫米大小的眼贴，上面包含微针阵列，这些微针以有控制的方式将药物递送至眼球。微针会逐渐溶解，缓慢地将药物释放到周围环境里面。在小鼠实验中，研究人员用拇指短暂轻压，将上述眼贴贴在小鼠眼表面。作者使用角膜新生血管作为模型，证明利用眼贴递送单克隆抗体DC101进行单次治疗后，小鼠的新生血管面积减小了约90%。相比之下，即使使用更高剂量的滴眼液，也无法取得显著的治疗效果。

图2：使用微型贴剂组合疗法的炎症评估。 碱烧伤2天后对小鼠眼睛进行不同的治疗，并在第7天检查疗效。图源：Than等

未来，还需要开展临床研究来评估这种新装置对人类的有效性和安全性。

摘要：Eye diseases and injuries impose a significant clinical problem worldwide. Safe and effective ocular drug delivery is, however, challenging due to the presence of ocular barriers. Here we report a strategy using an eye patch equipped with an array of detachable microneedles. These microneedles can penetrate the ocular surface tissue, and serve as implanted micro-reservoirs for controlled drug delivery. The biphasic drug release kinetics enabled by the double-layered micro-reservoirs largely enhances therapeutic efficacy. Using corneal neovascularization as the disease model, we show that delivery of an anti-angiogenic monoclonal antibody (DC101) by such eye patch produces ~90% reduction of neovascular area. Furthermore, quick release of an anti-inflammatory compound (diclofenac) followed by a sustained release of DC101 provides synergistic therapeutic outcome. The eye patch application is easy and minimally invasive to ensure good patient compliance. Such intraocular drug delivery strategy promises effective home-based treatment of many eye diseases.

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