全眼关注半氟烷烃:半氟烷烃滴眼液对干眼症患者泪膜稳定和给药影响的综合综述

Priyanka Agarwal, Alice Epitropoulos, Ian Gaddie, Anat Galor, Paul Karpecki, Eric Schmidt
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引用次数: 0

摘要

干眼病(DED)是一种常见的多因素眼部疾病,以泪膜不稳定、眼表炎症和患者不适为特征,对生活质量产生负面影响。由于药物生物利用度和患者耐受性差,传统疗法存在局限性。综述了半氟化烷烃(sfa)作为先进的眼部给药系统的应用,重点介绍了基于全氟丁基戊烷(PFBP)的环孢素a (CsA)滴眼液。强调SFAs对泪膜动力学、眼部生物利用度和患者报告结果影响的临床前和临床证据已被讨论。该综述汇编了截至2024年在同行评审期刊、数据库(包括PubMed、USPTO和会议摘要)中报告的临床前和临床研究结果。专家意见:sfa代表了眼部给药的范式转变。基于pfbp的滴眼液具有独特的物理化学特性,如无水特性、优异的涂抹性和稳定泪膜脂层的能力,解决了传统DED治疗相关的几个挑战。临床证据表明,基于pfbp的CsA滴眼液(VEVYE®)比含水CsA滴眼液起效更早,对DED的临床体征和症状有显著改善,患者耐受性高。正在进行的临床试验正在探索使用基于sfa的载体来治疗其他疾病,旨在克服药物递送限制。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
All eyes on semifluorinated alkanes: a comprehensive review of the influence of semifluorinated alkane eyedrops on tear film stabilization and drug delivery in dry eye disease.

Introduction: Dry eye disease (DED) is a prevalent and multifactorial ocular disorder characterized by tear film instability, ocular surface inflammation, and patient discomfort, negatively impacting the quality of life. Conventional therapies have limitations due to poor drug bioavailability and patient tolerability.

Areas covered: This review summarizes the application of semifluorinated alkanes (SFAs) as advanced ocular drug delivery systems, with a focus on perfluorobutylpentane (PFBP)-based cyclosporine A (CsA) eyedrops. Preclinical and clinical evidence highlighting the influence of SFAs on tear film dynamics, ocular bioavailability, and patient-reported outcomes has been discussed. The review compiles findings from preclinical and clinical studies reported in peer-reviewed journals and databases, including PubMed, USPTO, and conference abstracts up to 2024.

Expert opinion: SFAs represent a paradigm shift in ocular drug delivery. The unique physicochemical properties of PFBP-based eyedrops, such as their water-free nature, excellent spreadability, and ability to stabilize tear film lipid layer address several challenges associated with conventional DED therapies. Clinical evidence demonstrates that PFBP-based CsA eyedrops (VEVYE®) have an earlier onset of action than aqueous CsA eyedrops and show a significant improvement in the clinical signs and symptoms of DED with high patient tolerability. These properties of PFBP make it an excellent vehicle for ocular delivery and management of ocular surface disorders.

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