Schultz Clyde, Breaux Jason, Schentag Jerome, Morck Douglas
DirectContact LLC, Swampscott, Massachusetts 01907, USA.
Clin Exp Optom. 2011 Mar;94(2):212-8. doi: 10.1111/j.1444-0938.2010.00553.x. Epub 2010 Dec 22.
Despite pharmacological advances, delivery of drugs to the posterior segment of the eye remains problematic. We investigated the ability of hydrogel contact lenses to deliver small-molecule steroids, as well as larger biological molecules to the posterior segment.
Release characteristics of steroid-instilled lenses were studied in vitro. Drug delivery to the posterior segment of the eye was evaluated in a rabbit model, in which hydrogel contact lenses treated with diluted steroids (prednisolone or beclomethasone) were placed on rabbit corneas for four hours on days 1, 2, 5, 8 and 10. The amount of drug in plasma, posterior segment tissue and vitreous humour was measured with high-performance liquid chromatography-tandem mass spectrometry. In a further preliminary investigation, two rabbits were treated with ranibizumab.
The lenses released prednisolone and beclomethasone in saline over a six-hour period at a declining rate. Prednisolone was found in posterior segment tissue from six of six rabbits at concentrations ranging from 26.8 to 166 ng/g and in vitreous humour from two of six rabbits. Beclomethasone was detected in posterior segment tissue from three rabbits but was not found in the vitreous humour. Ranibizumab was detected in posterior segment tissue in a range from 0.19 ng/mL to 0.5183 ng/mL.
Hydrogel contact lenses are a non-invasive, periocular drug delivery device capable of achieving measurable drug levels in posterior segment tissue.
尽管药理学取得了进展，但将药物递送至眼后段仍然存在问题。我们研究了水凝胶隐形眼镜将小分子类固醇以及更大的生物分子递送至眼后段的能力。
对注入类固醇的隐形眼镜的释放特性进行了体外研究。在兔模型中评估药物向眼后段的递送情况，在第1、2、5、8和10天，将用稀释类固醇（泼尼松龙或倍氯米松）处理过的水凝胶隐形眼镜置于兔角膜上4小时。用高效液相色谱 - 串联质谱法测量血浆、眼后段组织和玻璃体液中的药物量。在进一步的初步研究中，对两只兔子用雷珠单抗进行治疗。
隐形眼镜在盐水中6小时内以递减速率释放泼尼松龙和倍氯米松。在6只兔子中的6只的眼后段组织中发现了泼尼松龙，浓度范围为26.8至166 ng/g，在6只兔子中的2只的玻璃体液中发现了泼尼松龙。在3只兔子的眼后段组织中检测到了倍氯米松，但在玻璃体液中未发现。在眼后段组织中检测到的雷珠单抗浓度范围为0.19 ng/mL至0.5183 ng/mL。
水凝胶隐形眼镜是一种非侵入性的眼周给药装置，能够在眼后段组织中达到可测量的药物水平。
