Lee V H, Robinson J R
University of Southern California, School of Pharmacy, Los Angeles.
J Ocul Pharmacol. 1986 Winter;2(1):67-108. doi: 10.1089/jop.1986.2.67.
Existing ocular drug delivery systems are fairly primitive and inefficient, but the stage is set for the rational design of newer and significantly improved systems. The focus of this review is on recent developments in topical ocular drug delivery systems relative to their success in overcoming the constraints imposed by the eye and to the improvements that have yet to be made. In addition, this review attempts to place in perspective the importance of pharmacokinetic modeling, ocular drug pharmacokinetic and bioavailability studies, and choice of animal models in the design and evaluation of these delivery systems. Five future challenges are perceived to confront the field. These are: (a) The extent to which the protective mechanisms of the eye can be safely altered to facilitate drug absorption, (b) Delivery of drugs to the posterior portion of the eye from topical dosing, (c) Topical delivery of macromolecular drugs including those derived from biotechnology, (d) Improved technology which will permit non-invasive monitoring of ocular drug movement, and (e) Predictive animal models in all phases of ocular drug evaluation.
现有的眼部给药系统相当原始且效率低下,但为更新且显著改进的系统进行合理设计的阶段已经就绪。本综述的重点是局部眼部给药系统的最新进展,涉及它们在克服眼部所施加的限制方面的成功情况以及尚未实现的改进。此外,本综述试图正确看待药代动力学建模、眼部药物药代动力学和生物利用度研究以及动物模型的选择在这些给药系统的设计和评估中的重要性。该领域预计将面临五个未来挑战。这些挑战是:(a) 眼部保护机制能够在多大程度上被安全改变以促进药物吸收,(b) 从局部给药将药物递送至眼后部,(c) 包括源自生物技术的药物在内的大分子药物的局部递送,(d) 能够允许对眼部药物移动进行非侵入性监测的改进技术,以及 (e) 在眼部药物评估的所有阶段中的预测性动物模型。