Eyeworld

DECEMBER 2019 | SUPPLEMENT TO EYEWORLD | 5 Supported by an unrestricted educational grant from EyePoint Pharmaceuticals, ImprimisRx, Ocular Therapeutix, and Omeros Edward Holland, MD Targeted drug delivery: Nanotechnology loteprednol T he development of better eye drops that can be ad- ministered less frequently may help reduce therapy adherence challenges. Not only could this help our postop patients but also those with chronic ophthalmic conditions. One strategy has been the formulation of mucus-pene- trating particle nanotechnology, which was applied to loteprednol. Twice-daily dosing Nanotechnology lotepred- nol etabonate suspension 1%, which was approved by the FDA in 2018, is the first twice-daily corticosteroid for postop pain and inflammation. It was developed based on the concept that smaller particles penetrate more effectively and By Edward Holland, MD can potentially reduce the drug concentration. Traditional suspension eye drops become trapped in the mucus layer, the defense system of the ocular surface, which prevents penetration of the drug. However, mucus-pene- trating particles pass through the mucus layer without disrupting it, resulting in better penetration and higher drug concentrations. In two multicenter, ran- domized clinical trials for FDA approval, at days 8 and 15, nanotechnology loteprednol significantly resolved pain and inflammation compared with the vehicle. 1 Resolution of pain to grade 0 was 43% on day 4, 56% on day 8, and 69% on day 15. Most cataract surgeons add a nonste- roidal anti-inflammatory, which is quite effective. We also need to know whether increasing the drug penetration will worsen side effects. However, loteprednol is a very good molecule and the only available ester steroid. Ester steroids usually do not in- crease IOP like ketone steroids do. This clinical trial showed that there was no significant difference in side effects com- pared with the control. Conclusion I believe better formulations, muco-adhesive technology, muco-penetrating particles, smaller drug particle size, and sustained-release technology will play an important role in managing pain postop with fewer drops. This strategy also would be beneficial in treating chronic diseases such as dry eye and glaucoma. n References 1. Kim T, et al. Safety and efficacy of twice daily administration of KPI-121 1% for ocular inflammation and pain following cataract surgery. Clin Oph- thalmol. 2019;13:69–86. Dr. Holland is director of the Cornea Service at the Cincinnati Eye Institute and professor of Ophthalmology at the University of Cincinnati. He can be contacted at eholland@holprovision.com. 4. Tyson S, et al. Multicenter random- ized phase 3 study of a sustained-re- lease intracanalicular dexametha- sone insert for treatment of ocular inflammation and pain after cataract surgery. J Cataract Refract Surg. 2019;45:204–12. 5. Noecker RJ, et al. Evaluating the physician and patient experience of a dexamethasone insert (0.4 mg) in patients having cataract surgery. Pre- sented at the ASCRS Annual Meeting. April 16, 2018; Washington, DC. Dr. Epitropoulos is clinical assis- tant professor at The Ohio State University Wexner Medical Center, co-founder of the Eye Center of Co- lumbus, and partner at Ophthalmic Surgeons & Consultants of Ohio. She can be contacted at aepitrop@ columbus.rr.com. continued from page 4 Inflammation Pain Loteprednol (%) Vehicle (%) Loteprednol (%) Vehicle (%) Day 4 43 25 Day 8 24 13 56 36 Day 15 50 27 69 48 Percentage of patients with complete resolution of anterior chamber cells and pain

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