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An Ilomastat-CD Eye Drop Formulation to Treat Ocular Scarring
Abeer H A Mohamed-Ahmed1, Alastair Lockwood1, He Li2
1UCL School of Pharmacy, London, United Kingdom 2UCL Institute of Ophthalmology, London, United Kingdom.
Investigative Ophthalmology & Visual Science
|July 11, 2017
Summary
This study developed a novel eye drop formulation using ilomastat-cyclodextrin (ilomastat-CD) for antiscarring therapy. The new formulation effectively delivered therapeutic concentrations of ilomastat to ocular tissues, showing potential for preventing post-surgical scarring.
Area of Science:
- Ophthalmology
- Pharmacology
- Biomaterials Science
Background:
- Scarring is a significant complication following ocular surgery, such as glaucoma filtration surgery.
- Matrix metalloproteinases (MMPs) play a role in tissue remodeling and fibrosis, making them targets for antifibrotic therapies.
Purpose of the Study:
- To develop a topical preparation of a matrix metalloproteinase inhibitor for antiscarring therapy.
- To formulate ilomastat, a broad-spectrum MMP inhibitor, with 2-hydroxypropyl-β-cyclodextrin for enhanced solubility and delivery.
Main Methods:
- Ilomastat was complexed with 2-hydroxypropyl-β-cyclodextrin (ilomastat-CD) in an aqueous solution.
- In vitro activity was assessed using fibroblasts in collagen, and ex vivo permeation through pig conjunctiva was evaluated.
- In vivo studies in rabbit eyes determined the ocular tissue distribution of ilomastat-CD via liquid chromatography-mass spectroscopy.
Main Results:
- Ilomastat-CD exhibited significantly enhanced aqueous solubility compared to uncomplexed ilomastat.
- The in vitro antifibrotic activity of ilomastat-CD was comparable to uncomplexed ilomastat.
- Topical application of ilomastat-CD eye drops resulted in therapeutic concentrations in rabbit ocular tissues and fluids.
Conclusions:
- Ilomastat-CD eye drops demonstrate potential as an effective antifibrotic agent for preventing ocular scarring.
- This formulation may be beneficial in settings like post-glaucoma surgery to reduce scar tissue formation.
