ADDRes Lab, Department of Food and Drug, University of Parma, Parco Area delle Scienze 27/a, 43124 Parma, Italy.
Department of Chemistry, Life Science and Environmental Sustainability, University of Parma, Parco Area delle Scienze 17/a, 43124 Parma, Italy.
Int J Pharm. 2023 May 10;638:122911. doi: 10.1016/j.ijpharm.2023.122911. Epub 2023 Apr 5.
Ocular drug delivery is challenging due to the poor drug penetration across ocular barriers and short retention time of the formulation at the application site. Films, applied as inserts or implants, can be used to increase residence time while controlling drug release. In this work, hydrophilic films made of hyaluronic acid and two kinds of PVA were loaded with dexamethasone (included as hydroxypropylcyclodextrin complex) and levofloxacin. This association represents one of the main treatments for the post cataract surgery management, and it is also promising for eye infections with pain and inflammation. Films were characterized in terms of swelling and drug release and were then applied to porcine eye bulbs and isolated ocular tissues. Film swelling leads to the formation of either a gel (3D swelling) or a larger film (2D swelling) depending on the type of PVA used. Films, prepared in an easy and scalable method, demonstrated high loading capacity, controlled drug release and the capability to deliver dexamethasone and levofloxacin to the cornea and across the sclera, to potentially target also the posterior eye segment. Overall, this device can be considered a multipurpose delivery platform intended for the concomitant release of lipophilic and hydrophilic drugs.
由于眼部屏障对药物的穿透性差以及制剂在应用部位的保留时间短，眼部药物输送具有挑战性。膜剂，如作为插入物或植入物，可以用于增加滞留时间，同时控制药物释放。在这项工作中，由透明质酸和两种 PVA 制成的亲水膜负载了地塞米松（包含作为羟丙基环糊精复合物）和左氧氟沙星。这种联合用药是白内障手术后管理的主要治疗方法之一，对于伴有疼痛和炎症的眼部感染也很有前景。对膜剂进行了溶胀和药物释放方面的特性研究，然后将其应用于猪眼球和离体眼部组织。根据所用 PVA 的类型，膜剂的溶胀会导致形成凝胶（3D 溶胀）或更大的膜（2D 溶胀）。该方法易于规模化，制备的膜剂具有高载药量、控释药物的能力，并且能够将地塞米松和左氧氟沙星递送到角膜和巩膜，有可能靶向眼部的后节。总的来说，这种装置可以被认为是一种多功能的给药平台，旨在同时释放亲脂性和亲水性药物。
