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

Abstract

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.

Keywords: Anti-inflammatory; bioavailability; cyclosporine; dry eye disease; perfluorobutylpentane; perfluorohexyloctane; semifluorinated alkanes.