Trans-eyelid distribution of epinastine to the conjunctiva following eyelid application in rabbits.

IF 2.1 3区 医学 Q2 OPHTHALMOLOGY
Japanese Journal of Ophthalmology Pub Date : 2024-09-01 Epub Date: 2024-05-25 DOI:10.1007/s10384-024-01070-6
Takaharu Mochizuki, Tatsuya Hata, Naoto Mori, Takashi Yamazaki, Takahisa Noto, Hidetoshi Mano
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引用次数: 0

Abstract

Purpose: To reveal the penetration of epinastine, an anti-allergic ophthalmic agent, into the eyelid and its distribution to the conjunctiva after administration of a cream formulation on rabbit eyelid skin.

Study design: Experimental study.

Methods: Rabbits were treated with 0.5% epinastine cream on hair-shaved eyelids, followed by preparation of eyelid tissue slices to determine spatial tissue distribution of epinastine by liquid chromatography-tandem mass spectrometry (LC-MS/MS) quantification using laser-microdissected tissues and desorption electrospray ionization mass spectrometry imaging (DESI-MSI). In addition, following either eyelid application of 0.5% epinastine cream or ocular instillation of 0.1% epinastine eye drops, concentration-time profiles of epinastine in the palpebral conjunctiva and bulbar conjunctiva were determined using LC-MS/MS.

Results: Laser microdissection coupled with LC-MS/MS analysis detected high concentrations of epinastine around the outermost layer of the eyelid at 0.5 h post-administration that gradually diffused deeper into the eyelid and was distributed in the conjunctival layer at 8 and 24 h post-administration. Similar time-dependent drug distribution was observed in high-spatial-resolution images obtained using DESI-MSI. Epinastine concentrations in the conjunctival tissues peaked at 4-8 h after administration of 0.5% epinastine cream and then decreased slowly over 72 h post-administration. In contrast, epinastine concentrations peaked quickly and decreased sharply after epinastine eye drop administration.

Conclusion: After the application of epinastine cream to the eyelid skin, epinastine gradually permeated the eyelid. The compound was retained in the conjunctiva for 8-24 h post-administration, indicating that epinastine cream is a promising long-acting formulation for treating allergic conjunctivitis.

Abstract Image

在兔子眼睑涂抹依匹斯汀后,依匹斯汀经眼睑分布到结膜。
目的:揭示抗过敏眼药依匹斯汀在兔眼睑皮肤上涂抹乳膏制剂后在眼睑的渗透及其在结膜的分布情况:研究设计:实验研究:方法:在剃掉毛发的兔眼睑上涂抹 0.5% 依匹斯汀乳膏,然后制备眼睑组织切片,利用激光微切片组织和解吸电喷雾离子化质谱成像(DESI-MSI),通过液相色谱-串联质谱(LC-MS/MS)定量分析确定依匹斯汀的空间组织分布。此外,在眼睑涂抹 0.5% 依匹斯汀乳膏或眼部滴入 0.1% 依匹斯汀滴眼液后,使用 LC-MS/MS 测定了睑结膜和球结膜中依匹斯汀的浓度-时间曲线:结果:激光显微切割结合 LC-MS/MS 分析发现,用药后 0.5 小时,眼睑最外层周围的依那斯汀浓度较高,用药后 8 小时和 24 小时,浓度逐渐向眼睑深处扩散,并分布在结膜层中。在使用 DESI-MSI 获得的高空间分辨率图像中也观察到了类似的时间依赖性药物分布。0.5% 依匹斯汀乳膏用药后 4-8 小时,结膜组织中的依匹斯汀浓度达到峰值,然后在用药后 72 小时内缓慢下降。相比之下,依匹斯汀滴眼液用药后,依匹斯汀浓度迅速达到峰值并急剧下降:结论:在眼睑皮肤上涂抹依匹斯汀乳膏后,依匹斯汀会逐渐渗入眼睑。结论:在眼睑皮肤上涂抹依匹斯汀乳膏后,依匹斯汀会逐渐渗透到眼睑中,在用药后的 8-24 小时内,该化合物一直保留在结膜中,这表明依匹斯汀乳膏是一种治疗过敏性结膜炎的长效制剂。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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来源期刊
CiteScore
4.80
自引率
8.30%
发文量
65
审稿时长
6-12 weeks
期刊介绍: The Japanese Journal of Ophthalmology (JJO) was inaugurated in 1957 as a quarterly journal published in English by the Ophthalmology Department of the University of Tokyo, with the aim of disseminating the achievements of Japanese ophthalmologists worldwide. JJO remains the only Japanese ophthalmology journal published in English. In 1997, the Japanese Ophthalmological Society assumed the responsibility for publishing the Japanese Journal of Ophthalmology as its official English-language publication. Currently the journal is published bimonthly and accepts papers from authors worldwide. JJO has become an international interdisciplinary forum for the publication of basic science and clinical research papers.
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