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08:44
Preparation, Administration, and Assessment of In Vivo Tissue-Specific Cellular Uptake of Fluorescent Dye-Labeled Liposomes
Published on: July 30, 2020
Repurposing glibenclamide for retinal protection: TUDCA-modified liposomes for ocular delivery
Sofia Dalla Lana1, Francesco Bertocchi2, Caterina Ricci3
1ADDRes Lab, Department of Food and Drug, University of Parma, Parco Area delle Scienze 27/a, 43124 Parma, Italy.
International Journal of Pharmaceutics
|July 24, 2026
Summary
This study developed a novel liposomal eye drop for glibenclamide, enhancing drug delivery for diabetic retinopathy and age-related macular degeneration. The formulation, improved with TUDCA, showed better penetration and sustained release, offering a promising new treatment option.
Area of Science:
- Ophthalmology
- Pharmaceutics
- Drug Delivery
Background:
- Glibenclamide, an oral diabetes drug, shows neuroprotective effects in ocular tissues.
- Diabetic retinopathy and age-related macular degeneration (AMD) are leading causes of vision loss.
- Local ocular delivery of glibenclamide could improve treatment efficacy and patient outcomes.
Purpose of the Study:
- To develop a topical liposomal formulation for ocular glibenclamide delivery.
- To enhance ocular bioavailability and achieve sustained drug release.
- To optimize liposome properties using tauroursodeoxycholic acid (TUDCA) for improved drug penetration.
Main Methods:
- Liposomes were formulated with and without TUDCA to optimize properties.
- Small-angle X-ray scattering (SAXS) analyzed vesicle deformability.
- Ex vivo permeation studies utilized porcine ocular tissues (cornea, conjunctiva, sclera).
- ARPE-19 cell lines assessed formulation tolerability.
Main Results:
- TUDCA incorporation increased liposome deformability and glibenclamide loading.
- TUDCA acted as an edge activator, enhancing drug penetration through ocular tissues.
- Liposomes accumulated in the sclera, creating a reservoir for sustained release.
- The glibenclamide liposomal formulation exhibited good tolerability in ARPE-19 cells.
Conclusions:
- TUDCA-modified liposomes are a promising system for ocular glibenclamide delivery.
- This formulation enhances drug penetration and provides sustained release for potential treatment of diabetic retinopathy and AMD.
- The developed liposomal formulation is safe and effective for ocular drug delivery.
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