Institute of Applied Ophthalmo-Biology (IOBA), University of Valladolid, 47011 Valladolid, Spain; Department of Pharmacology, Pharmacy and Pharmaceutical Technology, Faculty of Pharmacy, University of Santiago de Compostela (USC), Campus Vida, 15782 Santiago de Compostela, Spain.
Institute of Applied Ophthalmo-Biology (IOBA), University of Valladolid, 47011 Valladolid, Spain; Biomedical Research Networking Center on Bioengineering, Biomaterials and Nanomedicine (CIBER-BBN), Valladolid, Spain.
Int J Pharm. 2017 Oct 30;532(1):204-217. doi: 10.1016/j.ijpharm.2017.09.017. Epub 2017 Sep 8.
Topically-applied dosage forms, such eye drops, are the most used formulations in the treatment of ocular diseases. Nonetheless, because of the special protection of the eye associated with the ocular surface, drug bioavailability and subsequent therapeutic efficiency obtained with these conventional dosage forms are very low. Recently, novel drug delivery systems have been proposed to solve the main drawbacks of conventional formulations. Nanotechnology, and more specifically lipid nanoparticles, have emerged as promising "modified eyedrops" with the purpose of improving therapeutic efficiency without compromising drug safety and patient compliance. The purpose of this review is to offer an overview of lipid nanoparticles as feasible alternatives to the conventional topically-applied dosage forms. We discuss the main limitations of topical ocular drug delivery and describe how correctly designed lipid nanoparticles can be highly valuable tools to overcome the constraints imposed by the ocular surface. Special emphasis is placed on the description of production methods and bulk materials used in the development of lipid nanoparticles for ophthalmic use and how both issues will determine the physicochemical and biopharmaceutical properties of the developed nanosystems.
局部给药剂型，如滴眼剂，是治疗眼部疾病最常用的制剂。然而，由于眼睛与眼表面的特殊保护，这些常规剂型的药物生物利用度和随后的治疗效果非常低。最近，已经提出了新的药物传递系统来解决常规制剂的主要缺点。纳米技术，特别是脂质纳米粒，已经作为有前途的“改良滴眼剂”出现，目的是在不损害药物安全性和患者顺应性的情况下提高治疗效果。本文综述的目的是概述脂质纳米粒作为常规局部应用剂型的可行替代品。我们讨论了局部眼部药物传递的主要限制，并描述了如何正确设计的脂质纳米粒可以成为克服眼表面限制的极具价值的工具。特别强调了用于眼科用途的脂质纳米粒的生产方法和大量材料的描述，以及这两个问题将如何决定所开发的纳米系统的物理化学和生物制药特性。
