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维生素 E 负载隐形眼镜中奥洛他定的持续释放。

Sustained Delivery of Olopatadine from Vitamin-E Loaded Contact Lenses.

机构信息

Department of Chemical Engineering, University of Florida, Gainesville, Florida, USA.

Department of Chemical Engineering, Colorado School of Mines, Golden, Colorado, USA.

出版信息

J Ocul Pharmacol Ther. 2024 Mar;40(2):126-135. doi: 10.1089/jop.2023.0111.

Abstract

Topical antihistamines, such as olopatadine hydrochloride, an H1 receptor antagonist, are commonly prescribed for treating allergic conjunctivitis. Drug delivery via eye drops has many deficiencies including a short residence time due to tear drainage via the nasolacrimal duct, which results in a low bioavailability and potential for side effects. These deficiencies could be mitigated by a drug-eluting contact lens such as the recently approved ACUVUE THERAVISION™ WITH KETOTIFEN which is a daily disposable etafilcon, a drug-eluting contact lens with ketotifen (19 μg per lens). Here, we investigate the feasibility of designing a drug-eluting lens with sustained release of olopatadine for treating allergies using an extended wear lens. Nanobarrier depots composed of vitamin-E (VE) are formed through direct entrapment by ethanol-driven swelling. The drug-loaded lenses are characterized for transparency and water content. release is measured under sink conditions and fitted to a diffusion control release model to determine diffusivity and partition coefficient. studies indicate that ACUVUE OASYS and ACUVUE TruEye™ lenses loaded with ∼0.3 g of VE/g of hydrogel effectively prolong olopatadine dynamics by 7-fold and 375-fold, respectively. Incorporation of VE into the lenses retains visible light transmission and other properties. The VE incorporation in commercial lenses significantly increases the release duration offering the possibility of antiallergy extended wear lenses.

摘要

局部抗组胺药,如盐酸奥洛他定,一种 H1 受体拮抗剂,常用于治疗过敏性结膜炎。通过眼药水给药有许多缺陷,包括由于鼻泪管引流导致的泪液停留时间短,从而导致生物利用度低和潜在的副作用。通过药物洗脱隐形眼镜可以缓解这些缺陷,例如最近批准的 ACUVUE THERAVISION™ WITH KETOTIFEN,这是一种每日一次性的水凝胶隐形眼镜,含有 19μg 每片的酮替芬。在这里,我们研究了使用长戴隐形眼镜设计一种用于治疗过敏的奥洛他定缓释药物洗脱隐形眼镜的可行性。纳米屏障库由维生素 E (VE) 通过乙醇驱动的肿胀直接包埋形成。对载药隐形眼镜的透明度和含水量进行了表征。在水槽条件下进行释放测量,并拟合扩散控制释放模型,以确定扩散系数和分配系数。研究表明,ACUVUE OASYS 和 ACUVUE TruEye™隐形眼镜分别加载约 0.3g 的 VE/g 的水凝胶,可将奥洛他定的动力学有效延长 7 倍和 375 倍。VE 掺入隐形眼镜保留可见光透过率和其他性能。VE 掺入商业隐形眼镜显著增加了释放时间,为抗过敏长戴隐形眼镜提供了可能性。

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