Microparticle compositions and methods of use thereof

Microparticle formulations of PPARa agonists like A190, using PLGA and PEG, address the need for frequent injections by providing sustained release, enhancing treatment efficacy and compliance for retinal degeneration diseases.

WO2026128661A2 Publication Date: 2026-06-18VIRGINIA COMMONWEALTH UNIV
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Patent Information

Authority / Receiving Office
WO · WO
Patent Type
Applications
Current Assignee / Owner
VIRGINIA COMMONWEALTH UNIV
Filing Date
2025-12-11
Publication Date
2026-06-18

AI Technical Summary

⚠Technical Problem

Current treatments for retinal degeneration diseases like AMD, particularly neovascular AMD, require frequent intravitreal injections due to the short half-life of anti-VEGF drugs, imposing a significant burden on patients and healthcare systems, and there is no effective treatment for retinal degeneration.

⚗Method used

Development of microparticle formulations of PPARa agonists, such as A190, encapsulated in polymeric microparticles for sustained release, allowing a single injection every 6-12 months, utilizing polymers like PLGA and PEG to maintain effective drug concentrations in the eye.

🎯Benefits of technology

The microparticle formulations provide high drug loading and sustained release, reducing the frequency of injections, improving patient compliance, minimizing side effects, and prolonging therapeutic efficacy for retinal degeneration diseases.

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Abstract

Microparticulate (MP) formulations formed from one or more poly(hydroxyacid) polymers having a molecular weight ranging from 5kD to 60kD, and one or more active agents are injected into the eye of a subject to address eye disorders. The MP formulations assure high drug loading and extended delivery of the active agent of six to twelve months. The active agents may include peroxisome proliferator-activated receptor alpha (PPARα) signaling agonists such as PPARα agonist A190 (IUPAC name 3-((4-((4-fluorobenzyl)oxy)- 3- methylbenzyl)amino)benzoic acid). The formulations have therapeutic and protective effects against retinal degeneration diseases such as age-related macular degeneration (AMD), but may also be used for treating or relieving the symptoms of retinal inflammation, retinal neovascularization, retinal vascular leakage, retinopathy of prematurity (ROP), diabetic retinopathy (DR), and diabetic macular edema (DME).
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