Buchanan Ocular Therapeutics Unit, Department of Ophthalmology, New Zealand National Eye Centre, Faculty of Medical and Health Sciences, University of Auckland, Private Bag 92019, Auckland 1142, New Zealand; School of Pharmacy, Faculty of Medical and Health Sciences, University of Auckland, Private Bag 92019, Auckland, New Zealand.
School of Pharmacy, Faculty of Medical and Health Sciences, University of Auckland, Private Bag 92019, Auckland, New Zealand.
J Control Release. 2014 Dec 28;196:208-21. doi: 10.1016/j.jconrel.2014.09.030. Epub 2014 Oct 13.
Efficient drug delivery to the posterior segment of the eye is a challenging task for the formulation scientist. Current treatment of chronic back-of-the-eye conditions requires frequent intravitreal injections of drug containing solutions due to the short half-life and limited tissue permeation of the administered molecules. Sustained release ocular delivery systems offering reduced administration frequencies have therefore gained popularity over recent years with a few implants already on the market and many more in the pipeline. However, current implants generally release drug at a predetermined rate without the ability to alter release rates. As required drug concentrations may change over the course of treatment due to the individual patient's clinical response, implants from which release rates can be tuned could optimize treatment efficacy. This article provides an overview of diseases of the posterior segment of the eye, describes currently available implants to treat such conditions and discusses advantages and disadvantages of various implant locations. Finally, stimuli-responsive drug delivery technologies that have been investigated for, or have the potential to be applied to, drug delivery to the back of the eye will be discussed. Emphasis is hereby placed on polymeric implants responsive to an electric current, light or a magnetic field to achieve tunable drug release.
将药物有效地递送至眼部后段是制剂科学家面临的一项挑战。由于所给予的分子半衰期短且组织渗透性有限,目前治疗慢性眼后段疾病需要频繁进行玻璃体内注射含药物的溶液。近年来,由于减少给药频率的缓释眼部给药系统受到欢迎,已有少数几款植入物上市,还有更多的在研发中。然而,目前的植入物通常以预定的速度释放药物,而没有改变释放速度的能力。由于个体患者的临床反应,所需的药物浓度可能会在治疗过程中发生变化,因此能够调整释放速度的植入物可以优化治疗效果。本文概述了眼部后段疾病,描述了目前用于治疗此类疾病的植入物,并讨论了各种植入位置的优缺点。最后,本文讨论了已经针对眼部后段药物递送进行研究或有潜力应用于该领域的响应性药物递送技术。本文特别强调了对电流、光或磁场有响应的聚合物植入物,以实现可调节的药物释放。