Biophysics and Laser Science Unit, Research Institute of Ophthalmology, Giza, Egypt.
PLoS One. 2019 Feb 21;14(2):e0212588. doi: 10.1371/journal.pone.0212588. eCollection 2019.
Acetozolamide-ACZ, carbonic anhydrase inhibitor- is still the most effective systemic drug for glaucoma treatment. Due to its limited ocular bioavailability, topical formulations are not available yet. This study introduces within the framework of nanotechnology three nanopreparations of acetozolamide for topical application, one of them is liposomal phospholipid vehicle and the other two preparations are propolis and Punica granatum (pomegranate). The hypotensive effect of these different nanopreparations in lowering the increased intraocular pressure that was induced in experimental rabbits is monitored for 130 hrs. Structural characteristics of the optic nerve dissected from all involved groups were studied by Fourier transfrom infrared spectroscopy. The obtained results indicate the impact of the topically applied acetozolamide nanopreparations in lowering the intraocular pressure to its normotensive control value. On the other hand, the optic nerve characteristics were found to be dependent on the way acetozolamide introduced. Glaucoma affects structural components that contain OH group and increases β-turns of the protein secondary structure while, reducing the content of both α-helix and Turns. In the same context, liposomal-acetozolamide and propolis nanopreparations protecting the optic nerve protein secondary structure from these changes associated with glaucoma.
乙酰唑胺(ACZ)是一种碳酸酐酶抑制剂,仍是治疗青光眼最有效的全身药物。由于其眼部生物利用度有限,目前还没有局部用制剂。本研究在纳米技术的框架内介绍了三种用于局部应用的乙酰唑胺纳米制剂,其中一种是脂质体磷脂载体,另外两种制剂是蜂胶和石榴(石榴)。通过傅立叶变换红外光谱研究了从所有涉及组分离出的视神经的结构特征。监测这些不同纳米制剂在 130 小时内降低实验兔眼内压升高的降压效果。结果表明,局部应用乙酰唑胺纳米制剂可降低眼内压至正常血压控制值。另一方面,发现视神经特征取决于引入乙酰唑胺的方式。青光眼影响含有 OH 基团的结构成分,并增加蛋白质二级结构的β-转角,同时降低α-螺旋和转角的含量。在同样的背景下,脂质体-乙酰唑胺和蜂胶纳米制剂可保护视神经蛋白二级结构免受与青光眼相关的这些变化的影响。