Abdelmonem Rehab, Elhabal Sammar F, Abdelmalak Nevine S, El-Nabarawi Mohamed A, Teaima Mahmoud H
Department of Industrial Pharmacy, College of Pharmacy, Misr University for Science and Technology (MUST), 6th of October City, Giza 12566, Egypt.
Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Modern University for Technology and Information (MTI), Mokattam, Cairo 11571, Egypt.
Pharmaceutics. 2021 Feb 5;13(2):221. doi: 10.3390/pharmaceutics13020221.
Acetazolamide (ACZ) is a diuretic used in glaucoma treatment; it has many side effects. Carvedilol (CAR) is a non-cardioselective beta-blocker used in the treatment of elevated intraocular pressure; it is subjected to the first-pass metabolism and causes fluids accumulation leading to edema. This study focuses on overcoming previous side effects by using a topical formula of a combination of the two previous drugs. Sixty formulations of niosomes containing Span 20, Span 60, Tween 20, and Tween 60 with two different ratios were prepared and characterized. Formulation with the lowest particle size (416.30 ± 0.23), the highest zeta potential (72.04 ± 0.43 mv), and the highest apparent coefficient of corneal permeability (0.02 ± 0.29 cm/h) were selected. The selected formula was incorporated into the gel using factorial design 2. Niosomes (acetazolamide/carvedilol) consisting of Span 60 and cholesterol in the molar ratio (7:6), HMPC, and carbopol with two different ratios were used. The selected formula was subjected to an in vivo study of intraocular pressure in ocular hypertensive rabbits for 60 h. The sustained gel formula of the combination decreased (IOP) to normal after 1 h and sustained efficacy for 4 days. Histological analysis of rabbit eyeballs treated with the selected formula showed improvement in glaucomatous eye retinal atrophy.
乙酰唑胺（ACZ）是一种用于青光眼治疗的利尿剂；它有许多副作用。卡维地洛（CAR）是一种非选择性β受体阻滞剂，用于治疗眼压升高；它会经历首过代谢并导致液体蓄积，进而引起水肿。本研究的重点是通过使用这两种药物组合的局部配方来克服先前的副作用。制备并表征了60种含有司盘20、司盘60、吐温20和吐温60且比例不同的两种脂质体配方。选择了粒径最小（416.30±0.23）、zeta电位最高（72.04±0.43 mv）和角膜表观渗透系数最高（0.02±0.29 cm/h）的配方。使用析因设计2将所选配方加入凝胶中。使用摩尔比为（7:6）的司盘60和胆固醇、羟丙基甲基纤维素（HMPC）以及两种不同比例的卡波姆组成的脂质体（乙酰唑胺/卡维地洛）。对所选配方进行了对高眼压兔眼内压60小时的体内研究。该组合的缓释凝胶配方在1小时后将眼压（IOP）降至正常，并持续有效4天。用所选配方处理的兔眼球的组织学分析显示青光眼性视网膜萎缩有所改善。
