Department of Pharmaceutics, L. M. College of Pharmacy, Ahmedabad, India.
Deparment of Pharmacology, L. M. College of Pharmacy, Ahmedabad, India.
J Biomater Sci Polym Ed. 2024 Dec;35(18):2884-2908. doi: 10.1080/09205063.2024.2391233. Epub 2024 Aug 19.
This study aims to formulate and evaluate Eudragit nanoparticles-laden hydrogel contact lenses for controlled delivery of acetazolamide (ACZ) using experimental design. Eudragit S-100 was selected for the preparation of nanoparticles. The optimization of Eudragit S100 concentration (X1), polyvinyl alcohol concentration (X2), and the sonication time (X3) was attempted by applying a central composite experimental design. Mean size of nanoparticles (nm), percent drug release and drug leaching from the ACZ-ENs laden contact lens were considered as dependent variables. Nanoparticles-laden contact lens was prepared through the direct loading method and characterized. Optimum check-point formulation was selected based on validated quadratic polynomial equations developed using response surface methodology. The optimized formulation of ACZ-ENs exhibited spherical shape with a size of 244.3 nm and a zeta potential of -13.2 mV. The entrapment efficiency of nanoparticles was found to be 82.7 ± 1.21%. Transparent contact lenses loaded ACZ-ENs were successfully prepared using the free radical polymerization technique. ACZ-ENs incorporated in contact lens exhibited a swelling of 83.4 ± 0.82% and transmittance of 80.1 ± 1.23%. ACZ-ENs showed a significantly lower burst release of the drug when incorporated in the contact lens and release was sustained over a period of 24 h. The sterilized formulation of ACZ-ENs laden contact lens did not show any sign of toxicity in rabbit eyes. ACZ-ENs incorporated in contact lens could be considered as a potential alternative in glaucoma patients due to their ability to provide sustained drug release and thus enhance patient compliance.
本研究旨在通过实验设计,制备并评价载有乙酰唑胺(ACZ)的 Eudragit 纳米粒子水凝胶隐形眼镜,以实现药物的控释。选择 Eudragit S-100 制备纳米粒子。通过应用中心复合实验设计,尝试优化 Eudragit S100 浓度(X1)、聚乙烯醇浓度(X2)和超声时间(X3)。纳米粒子的平均粒径(nm)、药物释放百分比和 ACZ-ENs 载药隐形眼镜的药物浸出率被视为因变量。通过直接负载法制备载药隐形眼镜并进行了表征。基于响应面法建立的验证二次多项式方程,选择最佳检查点配方。优化后的 ACZ-ENs 呈球形,粒径为 244.3nm,zeta 电位为-13.2mV。纳米粒子的包封效率为 82.7±1.21%。采用自由基聚合技术成功制备了载有 ACZ-ENs 的透明隐形眼镜。载有 ACZ-ENs 的隐形眼镜具有 83.4±0.82%的溶胀率和 80.1±1.23%的透光率。当将 ACZ-ENs 掺入隐形眼镜中时,其药物释放呈现出明显的低突释效果,且可持续释放 24 小时。经灭菌处理的载有 ACZ-ENs 的隐形眼镜在兔眼上未显示出任何毒性迹象。载有 ACZ-ENs 的隐形眼镜可被视为青光眼患者的潜在替代治疗方法,因为其具有提供持续药物释放的能力,从而提高了患者的依从性。