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Neuroprotective effect of melatonin loaded in ethylcellulose nanoparticles applied topically in a retinal degeneration model in rabbits.
Experimental Eye Research ( IF 3.4 ) Pub Date : 2020-09-06 , DOI: 10.1016/j.exer.2020.108222
Carolina D V Bessone 1 , Sofia M Martinez 1 , José D Luna 2 , Marilyn A Marquez 2 , María L Ramírez 1 , Daniel A Allemandi 1 , Ágata R Carpentieri 3 , Daniela A Quinteros 1
Affiliation  

We are reporting for the first time the synthesis and application of an innovative nanometric system for the controlled topic release of melatonin in the retina. The ethylcellulose nanocapsules were characterized by diverse physicochemical techniques (scanning electron microscopy, zeta potential, hydrodynamic diameters) and an in vitro release study was done. A complete ex vivo and in vivo trans-corneal permeation and an irritation study were carried out with the new formulations in albino rabbits, to which a retinal degenerative model was induced. The results obtained demonstrate that the in vitro release of melatonin (1 mg/mL and 2 mg/mL) transported by nanocapsules is slower when compared to a solution of melatonin. Greater penetration of melatonin through the cornea was demonstrated by ex vivo and in vivo tests. This can be attributable to an enhanced neuroprotective effect of melatonin on retinal ganglion cells when it is included in ethylcellulose nanocapsules compared to a solution of melatonin. These outstanding findings add promising new perspectives to current knowledge about administrations using nano-technological tools in the treatment of neurodegenerative diseases at the ocular level.



中文翻译:

褪黑素负载在乙基纤维素纳米颗粒中的神经保护作用局部应用于兔视网膜变性模型。

我们首次报道了褪黑激素在视网膜中受控释放的创新纳米系统的合成和应用。乙基纤维素纳米胶囊通过多种物理化学技术(扫描电子显微镜,ζ电势,流体力学直径)表征,并进行了体外释放研究。用新配方在白化兔中进行了完整的离体和体内透角膜渗透和刺激研究,诱导了视网膜变性模型。获得的结果表明,与褪黑激素溶液相比,纳米胶囊运输的褪黑激素的体外释放速度(1 mg / mL和2 mg / mL)更慢。体外和体内试验证明褪黑激素可通过角膜更大的渗透。与褪黑激素溶液相比,褪黑激素包含在乙基纤维素纳米胶囊中时,这可归因于褪黑激素对视网膜神经节细胞的神经保护作用增强。这些出色的发现为使用纳米技术工具治疗眼部神经退行性疾病的当前管理知识增添了新的前景。

更新日期:2020-09-14
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