Research Institute for Medicines (iMed.ULisboa), Faculty of Pharmacy, Universidade de Lisboa, Portugal; CIISA - Centre for Interdisciplinary Research in Animal Health, Faculty of Veterinary Medicine, Universidade de Lisboa, Portugal.
CIISA - Centre for Interdisciplinary Research in Animal Health, Faculty of Veterinary Medicine, Universidade de Lisboa, Portugal.
Int J Pharm. 2021 Sep 5;606:120873. doi: 10.1016/j.ijpharm.2021.120873. Epub 2021 Jul 9.
Over the last years, the scientific interest about topical ocular delivery targeting the posterior segment of the eye has been increasing. This is probably due to the fact that this is a non-invasive administration route, well tolerated by patients and with fewer local and systemic side effects. However, it is a challenging task due to the external ocular barriers, tear film clearance, blood flow in the conjunctiva and choriocapillaris and due to the blood-retinal barriers, amongst other features. An enhanced intraocular bioavailability of drugs can be achieved by either improving corneal permeability or by improving precorneal retention time. Regarding this last option, increasing residence time in the precorneal area can be achieved using mucoadhesive polymers such as xyloglucan, poly(acrylate), hyaluronic acid, chitosan, and carbomers. On the other hand, colloidal particles can interact with the ocular mucosa and enhance corneal and conjunctival permeability. These nanosystems are able to deliver a wide range of drugs, including macromolecules, providing stability and improving ocular bioavailability. New pharmaceutical approaches based on nanotechnology associated to bioadhesive compounds have emerged as strategies for a more efficient treatment of ocular diseases. Bearing this in mind, this review provides an overview of the current mucoadhesive colloidal nanosystems developed for ocular topical administration, focusing on their advantages and limitations.
近年来,人们对靶向眼部后段的局部眼用制剂的研究兴趣日益增加。这可能是因为这种非侵入性给药途径患者易于接受,且局部和全身不良反应较少。然而,由于眼部外部屏障、泪膜清除、结膜和脉络膜的血流以及血视网膜屏障等特点,这是一项极具挑战性的任务。通过提高角膜通透性或延长药物在眼前部的滞留时间,可以提高药物的眼内生物利用度。关于后一种选择,可以使用粘弹性聚合物(如木葡聚糖、聚丙烯酸、透明质酸、壳聚糖和卡波姆)来增加在眼前部的停留时间,从而延长在眼前部的滞留时间。另一方面,胶体颗粒可以与眼黏膜相互作用,增强角膜和结膜的通透性。这些纳米系统能够递送包括大分子在内的多种药物,提供稳定性并提高眼内生物利用度。基于纳米技术并与生物黏附化合物相结合的新型药物制剂方法已成为治疗眼部疾病的更有效策略,本文综述了目前开发的用于局部眼用给药的粘弹性胶体纳米系统,重点介绍了它们的优缺点。