Liposome Encapsulation Enhances Ripasudil Therapeutic Efficacy Against Proliferative Vitreoretinal Diseases: Implications in Advanced Ocular Treatment

PMCID: PMC12178431

PMID: 40525920

DOI: 10.1167/iovs.66.6.56

Journal: Investigative ophthalmology & visual science

Publication Date: 2025-6-17

Authors: Ji R, Ishikawa K, Tan W, Mori K, Tsukamoto R, et al.

Key Points

• Liposomal encapsulation of ripasudil dramatically improves drug retention and targeted delivery in ocular tissues
• Lipo-Ripa demonstrated 146-fold increased vitreous concentration and sustained therapeutic effects compared to free ripasudil
• Offers a promising, non-toxic therapeutic approach for managing proliferative vitreoretinal diseases with potential for early intervention

Summary

This innovative study addresses the critical challenge of managing intraocular fibrosis in proliferative vitreoretinal diseases like proliferative vitreoretinopathy (PVR) and neovascular age-related macular degeneration (nAMD). By developing a liposomal encapsulation of ripasudil (Lipo-Ripa), a Rho-kinase inhibitor, researchers demonstrated a novel approach to enhance drug delivery and therapeutic efficacy in ocular tissues.

The researchers systematically evaluated Lipo-Ripa's pharmacokinetic properties, showing remarkable improvements in drug retention, cellular uptake, and sustained release compared to free ripasudil. In preclinical models, Lipo-Ripa significantly reduced subretinal fibrosis and suppressed disease progression, with in vivo studies revealing approximately 146-fold increased area under the curve in vitreous tissues and sustained therapeutic effects for up to 28 days after a single intravitreal injection.