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全氟己基辛烷眼药水与0.1%无水环孢素眼药水治疗干眼症的鉴别:临床前和临床特征综述

Differentiating Between Perfluorohexyloctane Ophthalmic Solution and Water-Free Cyclosporine Ophthalmic Solution 0.1% for Dry Eye Disease: A Review of Preclinical and Clinical Characteristics.

作者信息

Periman Laura M, White Darrell E, Katsev Douglas

机构信息

Periman Eye Institute, West Harrison Plaza North Tower, 100 W Harrison St Tower, Suite 360, Seattle, WA, 98119, USA.

Skyvision Centers, Westlake, OH, USA.

出版信息

Ophthalmol Ther. 2025 Feb;14(2):283-293. doi: 10.1007/s40123-024-01076-w. Epub 2025 Jan 7.

Abstract

Perfluorohexyloctane ophthalmic solution (Miebo) and water-free cyclosporine ophthalmic solution 0.1% (Vevye) are recently approved treatments for dry eye disease (DED). Perfluorohexyloctane (PFHO) uses a novel approach to treat evaporative DED, whereas water-free cyclosporine (CsA 0.1%) is formulated to increase ocular delivery of its active ingredient to improve tear production. The two medications utilize the distinctive properties of two different semifluorinated alkanes (SFAs) to elicit their therapeutic effects. PFHO consists of 100% active ingredient and forms a monolayer on the surface of the tear film to inhibit evaporation. CsA 0.1% utilizes a vehicle consisting of perfluorobutylpentane (PFBP) and ethanol to facilitate delivery of cyclosporine to ocular tissues. The structure of these SFAs determines their differing behaviors and functions. The longer chain length of PFHO results in a slower evaporation rate and facilitates formation of a stable monolayer on the ocular surface. In vitro, PFHO demonstrated a substantially lower evaporation rate versus PFBP or human meibum, as well as a significantly longer ocular surface residence time. Ex vivo, PFHO demonstrated a longer ocular surface residence time than PFBP. The shorter chain length of PFBP enables it to better solubilize cyclosporine and improve drug delivery to ocular tissues. Although both of these ophthalmic drops utilize SFAs, their differences-in physicochemical properties and the mechanisms by which they are understood to intervene in the DED cycle-are important considerations in treatment selection for patients with DED.

摘要

全氟己基辛烷眼药水(Miebo)和0.1%无水环孢素眼药水(Vevye)是最近获批用于治疗干眼病(DED)的药物。全氟己基辛烷(PFHO)采用一种新颖的方法来治疗蒸发型干眼病,而无水环孢素(0.1% CsA)的配方旨在增加其活性成分的眼部递送,以改善泪液分泌。这两种药物利用两种不同的半氟化烷烃(SFA)的独特性质来发挥其治疗作用。PFHO由100%活性成分组成,在泪膜表面形成单分子层以抑制蒸发。0.1% CsA利用一种由全氟丁基戊烷(PFBP)和乙醇组成的载体来促进环孢素向眼组织的递送。这些SFA的结构决定了它们不同的行为和功能。PFHO较长的链长导致其蒸发速率较慢,并有助于在眼表形成稳定的单分子层。在体外,与PFBP或人睑脂相比,PFHO的蒸发速率显著更低,且眼表停留时间明显更长。在离体实验中,PFHO的眼表停留时间比PFBP更长。PFBP较短的链长使其能够更好地溶解环孢素,并改善药物向眼组织的递送。尽管这两种眼药水都利用了SFA,但它们在物理化学性质以及据信它们干预干眼病周期的机制方面的差异,是干眼病患者治疗选择中的重要考虑因素。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d0ed/11754776/298e5be7a23e/40123_2024_1076_Fig1_HTML.jpg

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