Formulation to target delivery to the ciliary body and choroid via the suprachoroidal space of the eye using microneedles.
Formulation to target delivery to the ciliary body and choroid via the suprachoroidal space of the eye using microneedles.
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DOI：
10.1016/j.ejpb.2015.05.020
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发表时间：
2015-09
期刊：
影响因子：
--
通讯作者：
Prausnitz MR
中科院分区：
文献类型：
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作者：
Kim YC;Oh KH;Edelhauser HF;Prausnitz MR
在这项工作中，我们测试的假设，注射到脉络膜上腔的颗粒可以定位在注射部位或广泛分布在整个脉络膜上腔通过控制聚合物制剂的性能。将单个中空微针插入新西兰白色兔的巩膜中，并将悬浮在聚合物制剂中的不可生物降解的荧光标记的纳米颗粒和微粒注射到眼睛的脉络膜上间隙中。当在盐水中配制时，颗粒在注射后立即分布在脉络膜上腔的29% - 42%上。为了将颗粒散布在脉络膜表面的更大区域上，添加透明质酸以制备适度非牛顿溶液将颗粒散布增加至脉络膜上腔的100%。为了将颗粒定位在邻近睫状体的注射部位，强非牛顿聚合物溶液将颗粒定位到脉络膜上腔的8.3% - 20%，其在两个月的过程中表现出面积的小幅增加。该研究证明了使用聚合物制剂在脉络膜上腔内的靶向颗粒递送，所述聚合物制剂在整个脉络膜表面上散布颗粒或在注射后将它们定位在睫状体附近。
In this work, we tested the hypothesis that particles injected into the suprachoroidal space can be localized at the site of injection or broadly distributed throughout the suprachoroidal space by controlling polymeric formulation properties. Single hollow microneedles were inserted into the sclera of New Zealand White rabbits and injected non-biodegradable fluorescently tagged nanoparticles and microparticles suspended in polymeric formulations into the suprachorodial space of the eye. When formulated in saline, the particles were distributed over 29% - 42% of the suprachoroidal space immediately after injection. To spread particles over larger areas of the choroidal surface, addition of hyaluronic acid to make moderately non-Newtonian solutions increased particle spread to up to 100% of the suprachoroidal space. To localize particles at the site of injection adjacent to the ciliary body, strongly non-Newtonian polymer solutions localized particles to 8.3% – 20% of the suprachoroidal space, which exhibited a small increase in area over the course of two months. This study demonstrates targeted particle delivery within the suprachoroidal space using polymer formulations that spread particles over the whole choroidal surface or localized them adjacent to the ciliary body after injection.