Pigmented ocular tissues contain melanin within the intracellular melanosomes. Drugs bind to melanin at varying extent that ranges from no binding to extensive binding. Binding may lead to drug accumulation to the pigmented tissues and prolonged drug retention in the melanin containing cells. Therefore, melanin binding is an important feature that affects ocular drug delivery and biodistribution, but this topic has not been reviewed since 1998. In this review, we present current knowledge on ocular melanin, melanosomes and binding of drugs to pigmented cells and tissues. In vitro, in vivo and in silico methods in the field were critically evaluated, because the literature in this field can be confusing if the reader does not properly understand the methodological aspects. Literature analysis includes a comprehensive table of literature data on melanin binding of drugs. Furthermore, we aimed to give some insights beyond the current literature by making a chemical structure based classification model for melanin binding of drugs and kinetic simulations that revealed significant interplay between melanin binding and drug permeability across the melanosomal and plasma membranes. Overall, more mechanistic and systematic research is needed before the impact of melanin binding on ocular drug delivery can be properly understood and predicted.

色素沉着的眼组织在细胞内的黑素体内含有黑色素。药物以不同程度结合黑色素，范围从无结合到广泛结合。结合可能导致药物积累到色素沉着组织中，并延长药物在含黑色素细胞中的滞留时间。因此，黑色素结合是影响眼药物递送和生物分布的重要特征，但是自1998年以来就没有对此主题进行过综述。在本综述中，我们介绍了有关眼黑色素，黑素体以及药物与色素细胞和组织结合的最新知识。体外，体内和计算机模拟对该领域的方法进行了严格的评估，因为如果读者对方法方面的理解不正确，则该领域的文献可能会造成混淆。文献分析包括关于药物黑色素结合的文献数据的综合表。此外，我们旨在通过建立基于化学结构的药物黑色素结合分类模型和动力学模拟，提供超越当前文献的见解，该模拟模型揭示了黑色素结合与穿过黑素体和质膜的药物渗透性之间的显着相互作用。总体而言，在能够正确理解和预测黑色素结合对眼部药物传递的影响之前，需要进行更多的机械和系统的研究。