Santos Gonçalo, Delgado Esmeralda, Silva Beatriz, Braz Berta São, Gonçalves Lídia
Research Institute for Medicines (iMed.ULisboa), Faculty of Pharmacy, Universidade de Lisboa, 1649-003 Lisboa, Portugal.
CIISA-Centro de Investigação Interdisciplinar em Saúde Animal, Faculty of Veterinary Medicine, Universidade de Lisboa, 1300-477 Lisboa, Portugal.
Pharmaceutics. 2025 Mar 31;17(4):447. doi: 10.3390/pharmaceutics17040447.
Topical ophthalmic drug delivery targeting the posterior segment of the eye has become a key area of interest due to its non-invasive nature, safety, ease of application, patient compliance, and cost-effectiveness. However, achievement of effective drug bioavailability in the posterior ocular segment is a significant challenge due to unique ocular barriers, including precorneal factors and anatomical barriers, like the cornea, the conjunctiva, and the sclera. Successful ocular drug delivery systems require increased precorneal residence time and improved corneal penetration to enhance intraocular bioavailability. A promising strategy to overcome these barriers is incorporating drug penetration enhancers (DPEs) into formulations. These compounds facilitate drug delivery by improving permeability across otherwise impermeable or poorly permeable membranes. At the ocular level, they act through three primary mechanisms: breaking tear film stability by interfering with the mucous layer; disrupting membrane components such as phospholipids and proteins; and loosening epithelial cellular junctions. DPEs offer significant potential to improve bioavailability and therapeutic outcomes, particularly for drugs targeting the posterior segment of the eye. This review is focused on analyzing the current literature regarding the use of penetration enhancers in topical ocular drug delivery, highlighting their mechanisms of action and potential to revolutionize ophthalmic treatments.
由于其非侵入性、安全性、易于应用、患者依从性和成本效益，靶向眼后段的局部眼用药物递送已成为一个关键的研究领域。然而，由于独特的眼部屏障，包括角膜前因素和解剖学屏障，如角膜、结膜和巩膜，在眼后段实现有效的药物生物利用度是一项重大挑战。成功的眼部药物递送系统需要延长角膜前停留时间并提高角膜渗透性，以增强眼内生物利用度。克服这些屏障的一个有前景的策略是将药物渗透促进剂（DPEs）纳入制剂中。这些化合物通过改善跨原本不可渗透或渗透性差的膜的通透性来促进药物递送。在眼部水平，它们通过三种主要机制起作用：通过干扰粘液层破坏泪膜稳定性；破坏膜成分，如磷脂和蛋白质；以及松开上皮细胞连接。DPEs具有显著潜力来提高生物利用度和治疗效果，特别是对于靶向眼后段的药物。本综述着重分析当前关于在局部眼用药物递送中使用渗透促进剂的文献，突出其作用机制以及革新眼科治疗的潜力。
