经巩膜给药清除机制的评估。
Evaluation of clearance mechanisms with transscleral drug delivery.
作者信息
Lee Sung Jin, He Weiling, Robinson Shaun B, Robinson Michael R, Csaky Karl G, Kim Hyuncheol
机构信息
Department of Ophthalmology, College of Medicine, Soonchunhyang University, Seoul, South Korea.
出版信息
Invest Ophthalmol Vis Sci. 2010 Oct;51(10):5205-12. doi: 10.1167/iovs.10-5337. Epub 2010 May 19.
PURPOSE
The goal of this study was to examine elimination pathways when delivering subconjunctivally administered hydrophilic agents to the retinas of rat eyes.
METHODS
The distribution of sodium fluorescein released from an episcleral implant was compared in live and postmortem eyes. Elimination of the subconjunctivally administered hydrophilic agent IgG through blood and lymphatic vessels was investigated by immunohistochemistry. Additionally, lymphatic elimination of subconjunctivally injected sodium fluorescein was quantitatively evaluated.
RESULTS
NaFl released from an episcleral implant was successfully delivered to the subretinal space in the postmortem eye but failed to do so in the live eye. Immunohistochemical visualization of the conjunctival tissue demonstrated dense distribution of blood and lymphatic vessels while also confirming the elimination of subconjunctivally administered IgG through these same vessels. The lymphatic elimination rate after injection of 75.6 μg of a hydrophilic agent, sodium fluorescein, into the subconjunctival space was determined to be 105 ng/min between 30 and 60 minutes.
CONCLUSIONS
Conjunctival blood and lymphatic vessel elimination considerably limit transscleral hydrophilic drug delivery to the retina.
目的
本研究的目的是研究向大鼠眼视网膜结膜下注射亲水性药物时的消除途径。
方法
比较了巩膜上植入物释放的荧光素钠在活眼和死后眼中的分布情况。通过免疫组织化学研究结膜下注射的亲水性药物IgG通过血管和淋巴管的消除情况。此外，还对结膜下注射荧光素钠的淋巴消除情况进行了定量评估。
结果
巩膜上植入物释放的荧光素钠在死后眼中成功递送至视网膜下间隙，但在活眼中未能成功递送。结膜组织的免疫组织化学观察显示血管和淋巴管分布密集，同时也证实结膜下注射的IgG通过这些相同的血管被消除。向结膜下间隙注射75.6μg亲水性药物荧光素钠后，30至60分钟内的淋巴消除率为105 ng/分钟。
结论
结膜血管和淋巴管的消除显著限制了经巩膜向视网膜递送亲水性药物。
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