Vadlapudi Aswani Dutt, Patel Ashaben, Cholkar Kishore, Mitra Ashim K
Division of Pharmaceutical Sciences, School of Pharmacy, University of Missouri-Kansas City, 2464 Charlotte Street, Kansas City, MO 64108-2718, USA.
Recent Pat Biomed Eng. 2012 Apr 1;5(1):83-101. doi: 10.2174/1874764711205010083.
Advancements in the field and rising interest among pharmaceutical researchers have led to the development of new molecules with enhanced therapeutic activity. Design of new drugs which can target a particular pathway and/or explore novel targets is of immense interest to ocular pharmacologists worldwide. Delivery of suitable pharmacologically active agents at proper dose (within the therapeutic window) to the target tissues without any toxicity to the healthy ocular tissues still remain an elusive task. Moreover, the presence of static and dynamic barriers to drug absorption including the corneal epithelium (lipophilic), corneal and scleral stroma (hydrophilic), conjunctival lymphatics, choroidal vasculature and the blood-ocular barriers also pose a significant challenge for achieving therapeutic drug concentrations at the target site. Although many agents are currently available, new compounds are being introduced for treating various ocular diseases. Deeper understanding of the etiology and complex mechanisms associated with the disease condition would aid in the development of potential therapeutic candidates. Novel small molecules as well as complex biotechnology derived macromolecules with superior efficacy, safety and tolerability are being developed. Therefore, this review article provides an overview of existing drugs, treatment options, advances in emerging therapeutics and related recent patents for the treatment of ocular disorders such as glaucoma, age related macular degeneration (AMD) and uveitis.
该领域的进展以及制药研究人员日益浓厚的兴趣促使了具有增强治疗活性的新分子的开发。能够靶向特定途径和/或探索新靶点的新药设计引起了全球眼药理学家的极大兴趣。在不对健康眼组织产生任何毒性的情况下,以适当剂量(在治疗窗内)将合适的药理活性剂递送至靶组织,仍然是一项难以实现的任务。此外,药物吸收存在静态和动态屏障,包括角膜上皮(亲脂性)、角膜和巩膜基质(亲水性)、结膜淋巴管、脉络膜血管系统和血眼屏障,这也对在靶部位达到治疗药物浓度构成了重大挑战。尽管目前有许多药物可用,但仍不断有新化合物被引入用于治疗各种眼部疾病。对疾病病因和相关复杂机制的更深入理解将有助于开发潜在的治疗候选物。新型小分子以及具有卓越疗效、安全性和耐受性的复杂生物技术衍生大分子正在被研发。因此,这篇综述文章概述了现有药物、治疗选择、新兴疗法的进展以及治疗青光眼、年龄相关性黄斑变性(AMD)和葡萄膜炎等眼部疾病的相关近期专利。