Department of Physiology, "Iuliu Hatieganu" University of Medicine & Pharmacy, 400006 Cluj-Napoca, Romania.
Department of Pharmacology, Physiology and Physiopathology, "Iuliu Hatieganu" University of Medicine & Pharmacy, 400349 Cluj-Napoca, Romania.
Int J Mol Sci. 2023 Apr 28;24(9):8045. doi: 10.3390/ijms24098045.
The topical administration of medicines is the preferred route in ocular therapy, at least for the anterior segment of the eye. However, the eye's inherent functional and biological barriers all work against the active pharmaceutical ingredient (API) to efficiently reach the targeted retinal structures. The main objective of this article is to offer a systematic review of the scientific literature in recent years, focusing on the latest developments of topical treatment intended for retinal degenerative diseases. Database search returned 102 clinical studies, focused on topical treatment for age macular degeneration, macular edemas (in diabetic retinopathy, surgery related or in retinal dystrophies) or glaucoma. After the exclusion of low-powered studies and those combining vitreo-retinal surgery, 35 articles remained for analysis. Currently, the topical treatment of retinal degenerative diseases is limited by the difficulty to deliver effective drug concentrations to the posterior eye structures. However, in the case of drug classes like NSAIDs, the presence of certain molecular and metabolic features for specific representatives makes the topical administration currently feasible in several clinical contexts. For other drug classes, either a fine-tuning of the API's pharmacokinetic profile or the use of more advanced formulation strategies, such as rationally designed nanostructured drugs and vehicles, crystalline polymorphs or supramolecular complexes, could bring the much awaited breakthrough for a more predictable and controlled delivery towards the retinal structures and could eventually be employed in the future for the development of more effective ways of delivering drugs to the posterior eye, with the ultimate goal of improving their clinical efficacy.
局部给药是眼部治疗的首选途径,至少对于眼前节是如此。然而,眼睛固有的功能和生物学屏障都不利于活性药物成分(API)有效地到达靶向视网膜结构。本文的主要目的是对近年来的科学文献进行系统综述,重点介绍用于治疗视网膜退行性疾病的局部治疗的最新进展。数据库检索共返回 102 项临床研究,主要集中在针对年龄相关性黄斑变性、黄斑水肿(糖尿病性视网膜病变、手术相关或视网膜营养不良)或青光眼的局部治疗。排除低功率研究和将玻璃体内视网膜手术相结合的研究后,有 35 篇文章可供分析。目前,局部治疗视网膜退行性疾病受到限制,因为难以将有效药物浓度递送至眼后结构。然而,对于 NSAIDs 等药物类别,某些特定代表物具有特定的分子和代谢特征,使得局部给药在几种临床情况下目前是可行的。对于其他药物类别,要么调整 API 的药代动力学特征,要么使用更先进的制剂策略,如合理设计的纳米结构药物和载体、晶体多晶型或超分子配合物,可能会为更可预测和可控的向视网膜结构给药带来期待已久的突破,并最终可用于开发更有效的向眼后给药方法,最终目标是提高其临床疗效。