Seliniotaki Aikaterini K, Tziola Tatiana, Lithoxopoulou Maria, Tzamalis Argyrios, Ziakas Nikolaos, Mataftsi Asimina
2nd Department of Ophthalmology, School of Medicine, Faculty of Health Sciences, Aristotle University of Thessaloniki, Papageorgiou General Hospital, N.Efkarpia, Thessaloniki, 56429, Greece.
2nd Department of Neonatology, School of Medicine, Faculty of Health Sciences, Aristotle University of Thessaloniki, Thessaloniki, Greece.
Graefes Arch Clin Exp Ophthalmol. 2025 Feb 26. doi: 10.1007/s00417-025-06773-1.
Eyedrop instillation constitutes the most commonly used ocular drug delivery method that serves for both diagnostic and therapeutic purposes. Ocular disposition and bioavailability of instilled drugs depend on the anatomy and physiology of the ocular surface as well as the physicochemical properties of the active agent. Intraocular bioavailability is positively associated with the amount of drug available onto the ocular surface and the precorneal residence time. Concerns are raised regarding systemic absorption of the instilled drugs intraocularly, percutaneously, via the conjunctiva, through the nasolacrimal system, or through the nasal, oral, and gastrointestinal mucosa. Special considerations exist regarding the anatomical features and the limited pharmacokinetic data on the pediatric population that complicate further the efficacy and systemic toxicity of the instilled medications. Both preclinical and clinical studies propose the reduction of the instilled drop volume, in the form of microdrops, as a means to enhance intraocular bioavailability of topically applied drugs, while minimizing patient discomfort and systemic adverse events. We summarize existing data on the clinical application of microdrops in a wide age range, from preterm infants to elderly adults. Studies regarding microdrops of mydriatics and ocular hypotensives show promising results in optimizing the provided everyday care.
滴眼剂滴入是最常用的眼部给药方法，兼具诊断和治疗目的。滴入药物的眼部处置和生物利用度取决于眼表的解剖结构和生理功能以及活性剂的物理化学性质。眼内生物利用度与眼表可利用的药物量和角膜前滞留时间呈正相关。人们对滴入药物通过眼内、经皮、通过结膜、经鼻泪系统或通过鼻、口腔和胃肠道黏膜的全身吸收表示担忧。对于儿科人群的解剖特征和有限的药代动力学数据存在特殊考虑，这进一步使滴入药物的疗效和全身毒性变得复杂。临床前和临床研究均提出，以微滴形式减少滴入体积，作为提高局部应用药物眼内生物利用度的一种手段，同时将患者不适和全身不良事件降至最低。我们总结了关于微滴在从早产儿到老年人的广泛年龄范围内临床应用的现有数据。关于散瞳剂和降眼压剂微滴的研究在优化日常护理方面显示出有希望的结果。
