Tranilast, a lipophilic drug with various ophthalmic applications, was used as a model drug to establish the possibility of delivering lipophilic drugs through the eyelid skin. Pharmacokinetics and tissue distribution studies were conducted employing three application methods (topical application onto eyelid skin, eye drops, and intravenous injection in rats) to broaden the significance of delivering drugs through the eyelids. A two-compartment open model analysis was used for intravenous route while a non-compartmental evaluation was used for topical applications to estimate the pharmacokinetic parameters. Eyelid skin application, eye drops, and intravenous administration had mean residence times (MRTs) of 8.07, 1.79, and 3.25 h in the eyeball and 10.8, 1.29, and 2.97 h in the conjunctiva, correspondingly. In the eyeball, topical application of tranilast onto the eyelids corresponded to a 4.5- and 2.5-fold higher MRT compared with eye drops and intravenous administration, respectively. An 8.4- or 3.6-fold higher MRT was observed in the conjunctiva after topical application compared with eye drops or intravenous administration, respectively. This indicated a gradual penetration of tranilast into the eyeball and conjunctiva, subsequently a slow elimination from these target tissues.

Tranilast是一种具有多种眼科应用的亲脂性药物，它被用作模型药物，以确立通过眼睑皮肤递送亲脂性药物的可能性。通过三种施用方法（局部施用到眼睑皮肤，眼药水和大鼠静脉注射）进行了药代动力学和组织分布研究，以拓宽通过眼睑递送药物的重要性。两室开放模型分析用于静脉内途径，而无室评估用于局部应用以估计药代动力学参数。眼睑皮肤应用，滴眼液和静脉内给药的平均停留时间（MRT）在眼球中分别为8.07、1.79和3.25 h，在结膜中分别为10.8、1.29和2.97 h。在眼球中 曲尼司特在眼睑上的局部应用分别比滴眼液和静脉内给药分别高出4.5倍和2.5倍。与滴眼液或静脉内给药相比，局部应用后结膜中的MRT分别高8.4或3.6倍。这表明曲尼司特逐渐渗入眼球和结膜，随后从这些靶组织中缓慢清除。