Recent advances in ophthalmic drug delivery.
Recent advances in ophthalmic drug delivery.
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DOI：
10.4155/tde.10.40
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发表时间：
2010-09
影响因子：
4.2
通讯作者：
Lee VH
中科院分区：
文献类型：
--
作者：
Kompella UB;Kadam RS;Lee VH
众所周知，局部眼部药物的生物利用度很差，约为 5% 或更低。这是药物进入的有效多重屏障的结果，包括鼻泪管引流、上皮药物转运屏障和结膜脉管系统的清除。虽然目前可以通过 Vitrasert™（约 6 个月）、Retisert™（约 3 年）和 Iluvien™（约 3 年）等玻璃体内植入物将药物持续输送到眼后部，但目前还没有上市的输送系统可用于长期将药物输送到眼前节。本文的目的是总结对延长和改善局部给药的药物进入的兴趣的复苏。这些方法包括粘膜粘合剂、粘性聚合物载体、靶向转运蛋白的前药设计、靶向受体的功能化纳米颗粒、离子电渗疗法、泪点塞和隐形眼镜递送系统。其中一些传输系统可能有助于治疗影响眼睛后部的疾病。将其有效性与玻璃体内植入物（有效性上限）和经巩膜系统（有效性下限）进行比较。通过结合微透析和成像技术的最新进展来完善动物模型是扩展下一代创新眼部药物输送系统的设计、测试和评估核心知识的关键。
Topical ocular drug bioavailability is notoriously poor, in the order of 5% or less. This is a consequence of effective multiple barriers to drug entry, comprising nasolacrimal drainage, epithelial drug transport barriers and clearance from the vasculature in the conjunctiva. While sustained drug delivery to the back of the eye is now feasible with intravitreal implants such as Vitrasert™ (~6 months), Retisert™ (~3 years) and Iluvien™ (~3 years), currently there are no marketed delivery systems for long-term drug delivery to the anterior segment of the eye. The purpose of this article is to summarize the resurgence in interest to prolong and improve drug entry from topical administration. These approaches include mucoadhesives, viscous polymer vehicles, transporter-targeted prodrug design, receptor-targeted functionalized nanoparticles, iontophoresis, punctal plug and contact lens delivery systems. A few of these delivery systems might be useful in treating diseases affecting the back of the eye. Their effectiveness will be compared against intravitreal implants (upper bound of effectiveness) and trans-scleral systems (lower bound of effectiveness). Refining the animal model by incorporating the latest advances in microdialysis and imaging technology is key to expanding the knowledge central to the design, testing and evaluation of the next generation of innovative ocular drug delivery systems.