Department of Pharmacy, University of Pisa, Via Bonanno 33, 56126 Pisa, Italy.
Department of Pharmacy, University of Pisa, Via Bonanno 33, 56126 Pisa, Italy; Department of Pharmacy, University of Pisa, Via Bonanno 33, 56126 Pisa, Italy; Interdepartmental Research Center "Nutraceuticals and Food for Health", University of Pisa, Pisa 56100, Italy.
Adv Colloid Interface Sci. 2021 Feb;288:102342. doi: 10.1016/j.cis.2020.102342. Epub 2020 Dec 13.
Ocular diseases may be treated via different routes of administration, such as topical, intracameral, intravitreal, oral and parenteral. Among them the topical route is most accepted by patients, although it provides in many cases the lowest bioavailability. Indeed, when a topical formulation reaches the precorneal area, i.e., the drug absorption and/or action site, it is rapidly eliminated due to eye protection mechanisms such as blinking, basal and reflex tearing, and naso-lacrimal draining. To avoid this and to reduce the frequency of dosing, various strategies have been developed to prolong drug residence time after topical administration. These strategies include the use of viscosity increasing and mucoadhesive excipients as well as combinations thereof. From the drug delivery system point of view, liquid and semisolid formulations are preferred over solid formulations such as ocular inserts and contact lenses. Furthermore, liquid and semisolid formulations can contain nano- and microcarrier systems that contribute to a prolonged residence time. Within this review an overview about the different types of excipients and formulations as well as their performance in valid animal models and clinical trials is provided.
眼部疾病可以通过不同的给药途径治疗，例如局部、前房内、玻璃体内、口服和肠胃外。其中，局部途径最受患者接受，尽管在许多情况下它提供的生物利用度最低。事实上，当局部制剂到达角膜前区（即药物吸收和/或作用部位）时，由于眨眼、基础和反射性流泪以及鼻泪管引流等眼部保护机制，它会迅速被清除。为了避免这种情况并减少给药频率，已经开发了各种策略来延长局部给药后药物的停留时间。这些策略包括使用粘度增加和粘膜粘附赋形剂以及它们的组合。从药物传递系统的角度来看，液体和半固体制剂优于固体制剂，如眼内插入物和隐形眼镜。此外，液体和半固体制剂可以包含纳米和微载体系统，有助于延长停留时间。在本次综述中，概述了不同类型的赋形剂和制剂及其在有效动物模型和临床试验中的性能。
