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采用统计实验设计的载乙酰唑胺纳米粒子隐形眼镜的设计和优化用于控制眼部药物传递。

Design and optimization of acetazolamide nanoparticle-laden contact lens using statistical experimental design for controlled ocular drug delivery.

机构信息

Department of Pharmaceutics, L. M. College of Pharmacy, Ahmedabad, India.

Deparment of Pharmacology, L. M. College of Pharmacy, Ahmedabad, India.

出版信息

J Biomater Sci Polym Ed. 2024 Dec;35(18):2884-2908. doi: 10.1080/09205063.2024.2391233. Epub 2024 Aug 19.

DOI:10.1080/09205063.2024.2391233
PMID:39155730
Abstract

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.

摘要

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。

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