El-Feky Yasmin A, Mostafa Dalia A, Al-Sawahli Majid M, El-Telbany Rania Farag A, Zakaria Sherin, Fayez Ahmed M, Ahmed Kawkab A, Alolayan Ebtesam M, El-Telbany Dalia Farag A
Department of Pharmaceutics, Faculty of Pharmacy, Modern University for Technology and Information (MTI), Cairo, Egypt.
Department of Pharmaceutics, Faculty of Pharmacy, October University for Modern Sciences and Arts (MSA), Giza, Egypt.
J Pharm Pharmacol. 2020 May;72(5):682-698. doi: 10.1111/jphp.13239. Epub 2020 Mar 14.
To enhance bioavailability of timolol (TML) and utilize alternatives for traditional eye drops for more patient compliance, this study was aiming to develop biodegradable orally dissolving strips (ODSs) of TML for treatment of primary open-angle glaucoma (POAG).
Novel ODSs of TML were formulated and optimized using solvent casting method according to full factorial design (3 .2 ). TML ODSs were characterized with respect to many parameters. In-vivo test was carried out using four groups of 24 New Zealand albino rabbits. POAG was induced by subconjunctival treatment of betamethasone. Histopathological examination and oxidative stress markers assay were carried out.
The optimized formula (F9) exhibited a remarkably 15-s disintegration time and 96% dissolution rate after 10 min. The results revealed a potent significant inhibitory effect of the optimized TML ODS to reduce IOP in induced rabbits in comparison with control rabbits and TML eye drops-treated rabbits. The formula showed also high activity against oxidative stress and absence of histopathological changes in iridocorneal angle and cornea.
The ODSs could be a promising alternative delivery system for eye drops with more compliance to enhance delivery and therapeutic activity of TML in treatment of POAG.
为提高噻吗洛尔（TML）的生物利用度，并寻找传统滴眼液的替代剂型以提高患者依从性，本研究旨在开发用于治疗原发性开角型青光眼（POAG）的TML可生物降解口腔崩解片（ODS）。
根据全因子设计（3²），采用溶剂浇铸法制备并优化新型TML ODS。对TML ODS的多个参数进行了表征。使用四组共24只新西兰白化兔进行体内试验。通过结膜下注射倍他米松诱导POAG。进行了组织病理学检查和氧化应激标志物检测。
优化配方（F9）的崩解时间显著为15秒，10分钟后的溶出率为96%。结果显示，与对照兔和TML滴眼液治疗的兔相比，优化后的TML ODS对诱导兔降低眼压具有显著的抑制作用。该配方还显示出对氧化应激的高活性，且虹膜角膜角和角膜无组织病理学变化。
ODS可能是一种有前景的滴眼液替代给药系统，具有更高的依从性，可提高TML在POAG治疗中的给药和治疗活性。
