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Self-Assembling Elastin-Like Hydrogels for Timolol Delivery: Development of an Ophthalmic Formulation Against Glaucoma
Molecular Pharmaceutics ( IF 4.5 ) Pub Date : 2017-11-21 00:00:00 , DOI: 10.1021/acs.molpharmaceut.7b00615 Alicia Fernández-Colino 1 , Daniela A. Quinteros 2 , Daniel A. Allemandi 2 , Alessandra Girotti 1 , Santiago D. Palma 2 , F. Javier Arias 1
Molecular Pharmaceutics ( IF 4.5 ) Pub Date : 2017-11-21 00:00:00 , DOI: 10.1021/acs.molpharmaceut.7b00615 Alicia Fernández-Colino 1 , Daniela A. Quinteros 2 , Daniel A. Allemandi 2 , Alessandra Girotti 1 , Santiago D. Palma 2 , F. Javier Arias 1
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This work focuses on improving the effectiveness of current therapies against glaucoma by incorporating self-assembled polymers into the ophthalmic formulation. To that end, we first studied the influence of the dispersing medium on the mechanical performance of self-assembling elastin-like (EL) and silk-elastin-like (SEL) hydrogels by conducting rheological tests. These polymers were subsequently incorporated into the antiglaucoma formulation, which contains timolol maleate (TM) as active ingredient, and in vivo tests, namely adhesion tests and intraocular pressure measurements (IOP), were performed in New Zealand rabbits. An enhanced reduction in IOP due to the presence of the polymers was observed. Moreover, differences in the effectiveness between both EL- and SEL-hydrogels, which can be explained on the basis of the different rheological properties displayed by these two systems, were also encountered. The results point to the potential of this system as a basis for the development of an ophthalmic formulation against glaucoma.
中文翻译：
用于蒂莫洛尔递送的自组装类弹性蛋白水凝胶：针对青光眼的眼科制剂的开发
这项工作着眼于通过将自组装聚合物掺入眼科制剂中来提高当前抗青光眼治疗的有效性。为此，我们首先通过流变试验研究了分散介质对自组装类弹性蛋白（EL）和丝状弹性蛋白（SEL）水凝胶的机械性能的影响。随后将这些聚合物并入体内的抗青光眼制剂中，该制剂含有马来酸替莫洛尔（TM）作为有效成分。在新西兰兔中进行了测试，即附着力测试和眼内压测量（IOP）。观察到由于聚合物的存在，IOP降低的增强。此外，还遇到了EL和SEL水凝胶之间有效性的差异，这可以根据这两种系统显示出的不同流变特性来解释。结果表明该系统的潜力可作为开发抗青光眼的眼科制剂的基础。
更新日期：2017-11-22
中文翻译：
用于蒂莫洛尔递送的自组装类弹性蛋白水凝胶：针对青光眼的眼科制剂的开发
这项工作着眼于通过将自组装聚合物掺入眼科制剂中来提高当前抗青光眼治疗的有效性。为此，我们首先通过流变试验研究了分散介质对自组装类弹性蛋白（EL）和丝状弹性蛋白（SEL）水凝胶的机械性能的影响。随后将这些聚合物并入体内的抗青光眼制剂中，该制剂含有马来酸替莫洛尔（TM）作为有效成分。在新西兰兔中进行了测试，即附着力测试和眼内压测量（IOP）。观察到由于聚合物的存在，IOP降低的增强。此外，还遇到了EL和SEL水凝胶之间有效性的差异，这可以根据这两种系统显示出的不同流变特性来解释。结果表明该系统的潜力可作为开发抗青光眼的眼科制剂的基础。
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