Burhan Ayah Mohammad, Klahan Butsabarat, Cummins Wayne, Andrés-Guerrero Vanessa, Byrne Mark E, O'Reilly Niall J, Chauhan Anuj, Fitzhenry Laurence, Hughes Helen
Ocular Therapeutics Research Group, Pharmaceutical and Molecular Biotechnology Research Centre, Waterford Institute of Technology, X91 K0EK Waterford, Ireland.
Innovation, Therapy and Pharmaceutical Development in Ophthalmology (InnOftal) Research Group, Department of Pharmaceutics and Food Technology, Faculty of Pharmacy, Sanitary Research Institute of the San Carlos Clinical Hospital (IdISSC), Complutense University of Madrid, 28040 Madrid, Spain.
Pharmaceutics. 2021 Oct 14;13(10):1685. doi: 10.3390/pharmaceutics13101685.
Posterior segment eye diseases (PSEDs) including age macular degeneration (AMD) and diabetic retinopathy (DR) are amongst the major causes of irreversible blindness worldwide. Due to the numerous barriers encountered, highly invasive intravitreal (IVT) injections represent the primary route to deliver drugs to the posterior eye tissues. Thus, the potential of a more patient friendly topical route has been widely investigated. Mucoadhesive formulations can decrease precorneal clearance while prolonging precorneal residence. Thus, they are expected to enhance the chances of adherence to corneal and conjunctival surfaces and as such, enable increased delivery to the posterior eye segment. Among the mucoadhesive polymers available, chitosan is the most widely explored due to its outstanding mucoadhesive characteristics. In this review, the major PSEDs, their treatments, barriers to topical delivery, and routes of topical drug absorption to the posterior eye are presented. To enable the successful design of mucoadhesive ophthalmic drug delivery systems (DDSs), an overview of mucoadhesion, its theory, characterization, and considerations for ocular mucoadhesion is given. Furthermore, chitosan-based DDs that have been explored to promote topical drug delivery to the posterior eye segment are reviewed. Finally, challenges of successful preclinical to clinical translation of these DDSs for posterior eye drug delivery are discussed.
包括年龄相关性黄斑变性(AMD)和糖尿病视网膜病变(DR)在内的眼后段疾病(PSEDs)是全球不可逆失明的主要原因之一。由于面临众多障碍,高度侵入性的玻璃体内(IVT)注射是将药物输送到眼后段组织的主要途径。因此,人们广泛研究了一种对患者更友好的局部给药途径的潜力。粘膜粘附制剂可以减少角膜前清除率,同时延长角膜前停留时间。因此,预计它们会增加粘附在角膜和结膜表面的机会,从而增加向眼后段的药物递送量。在现有的粘膜粘附聚合物中,壳聚糖因其出色的粘膜粘附特性而得到最广泛的研究。在这篇综述中,介绍了主要的PSEDs、它们的治疗方法、局部给药的障碍以及药物向眼后段的局部吸收途径。为了成功设计粘膜粘附性眼科药物递送系统(DDSs),概述了粘膜粘附及其理论、表征以及眼部粘膜粘附的注意事项。此外,还综述了已探索的基于壳聚糖的DDSs,以促进向眼后段的局部药物递送。最后,讨论了这些用于眼后段药物递送的DDSs从临床前到临床成功转化面临的挑战。