Submicron formula ‘step forward’ in steroid therapy

Reviewed by Marguerite B. McDonald, MD

Loteprednol etabonate ophthalmic gel 0.38% (Lotemax SM, Bausch + Lomb) is a new iteration of the topical corticosteroid with a number of benefits for patients, said Marguerite B. McDonald, MD.

Approved by the FDA in February for the treatment of postoperative inflammation and pain following ocular surgery, the product is engineered with proprietary submicron technology that improves drug dissolution and penetration to target ocular tissues-resulting in treatment benefit with the convenience of twice-daily dosing.

Like its predecessor, loteprednol etabonate ophthalmic gel 0.5% (Lotemax, Bausch + Lomb), the agent is a non-settling gel in which the active ingredient remains homogenously distributed, obviating the need for patients to shake the container vigorously prior to instillation.

The submicron loteprednol etabonate gel is also gentle to the ocular surface because it contains two demulcents and is preserved with a very low concentration of benzalkonium chloride (0.003%), said Dr. McDonald, clinical professor of ophthalmology, NYU School of Medicine, and in private practice, Ophthalmic Consultants of Long Island, Lynbrook, NY.

She described submicron loteprednol etabonate gel 0.38% as “a huge step forward” in topical corticosteroid therapy. “The new submicron formulation of loteprednol etabonate gel brings the benefit of twice-daily dosing for a molecule that has a 20-year history documenting its efficacy and safety,” she said.

Particle science

The submicron-sized drug particles in loteprednol etabonate gel 0.38% have a median diameter of about 0.6 μm. By comparison, loteprednol etabonate gel 0.5% contains micronized drug particles that are about 3 μm in diameter.

Even though the new submicron formulation contains a lower concentration of loteprednol etabonate, it is effective with just twice-daily dosing because of its better drug dissolution and drug penetration characteristics compared with the 0.5% gel formulation, Dr. McDonald said.

The efficacy and safety of submicron loteprednol etabonate gel 0.38% for the treatment of postoperative inflammation and pain was investigated in a double-masked, vehicle-controlled randomized study that included 514 patients undergoing cataract surgery [Fong R, et al. J Cataract Refract Surg. 2018;44:1220-1229].

The proportions of patients with 1) resolution of anterior chamber cells and 2) no pain on postoperative day 8 were assessed as the primary outcome measures. Statistically significant differences favoring the BID and TID submicron loteprednol etabonate groups compared with vehicle were found in the analyses of both anterior chamber cell resolution (26.9% and 28.7% versus 9.3%) and absence of pain (73.7% and 73.1% versus 47.7%).

No safety concerns emerged in the submicron loteprednol etabonate treatment groups, and the treatment was well-tolerated.

Disclosures:

Marguerite B. McDonald, MD
E: margueritemcdmd@aol.com
Dr. McDonald is a consultant to Bausch + Lomb and other companies that market topical anti-inflammatory medications.