Kour Jagpreet, Kumari Neha, Sapra Bharti
Department of Pharmaceutical Sciences and Drug Research, Punjabi University, Patiala 147001, India.
Asian J Pharm Sci. 2021 Mar;16(2):175-191. doi: 10.1016/j.ajps.2020.08.002. Epub 2020 Sep 28.
Ocular drug delivery is one of the most attention-grabbing and challenging endeavors among the numerous existing drug delivery systems. From a drug delivery point of view, eye is an intricate organ to investigate and explore. In spite of many limitations, advancements have been made with the intention of improving the residence time or permeation of the drug in the ocular region. Poor bioavailability of topically administered drugs is the major issue pertaining to ocular drug delivery. Several efforts have been made towards improving precorneal residence time and corneal penetration, e.g. iontophoresis, prodrugs and ion-pairing, etc. Prodrug approach (chemical approach) has been explored by the formulation scientists to optimize the physicochemical and biochemical properties of drug molecules for improving ocular bioavailability. Formulation of ocular prodrugs is a challenging task as they should exhibit optimum chemical stability as well as enzymatic liability so that they are converted into parent drug after administration at the desired pace. This review will encompass the concept of derivatization and recent academic and industrial advancements in the field of ocular prodrugs. The progression in prodrug designing holds a potential future for ophthalmic drug delivery.
眼部药物递送是众多现有药物递送系统中最引人关注且具有挑战性的领域之一。从药物递送的角度来看，眼睛是一个复杂的有待研究和探索的器官。尽管存在许多限制，但为了提高药物在眼部区域的停留时间或渗透性，已经取得了一些进展。局部给药药物的生物利用度低是眼部药物递送的主要问题。人们已经做出了多种努力来提高药物在角膜前的停留时间和角膜渗透性，例如离子导入法、前体药物和离子对法等。制剂科学家们探索了前体药物方法（化学方法），以优化药物分子的物理化学和生化性质，从而提高眼部生物利用度。眼部前体药物的制剂是一项具有挑战性的任务，因为它们应表现出最佳的化学稳定性以及酶促反应性，以便在给药后能以所需的速度转化为母体药物。本综述将涵盖衍生化的概念以及眼部前体药物领域近期的学术和产业进展。前体药物设计的进展为眼科药物递送带来了潜在的未来发展前景。
