Loteprednol Etabonate (Submicron) Ophthalmic Gel 0.38%: A Review in Post-Operative Inflammation and Pain Following Ocular Surgery

Abstract

Loteprednol etabonate ophthalmic gel 0.38% (Lotemax ® SM; hereafter referred to as loteprednol etabonate gel 0.38%) is a topical ophthalmic corticosteroid approved in the USA for the treatment of post-operative inflammation and pain following ocular surgery. This formulation provides improved drug delivery compared with loteprednol etabonate micronized gel 0.5%, with a smaller drug particle size (in the submicron range) to improve dissolution and penetration into ocular tissues, meaning less loteprednol etabonate is required to exert therapeutic effect. In two multicentre, randomized phase III trials, significantly more loteprednol etabonate gel 0.38% than vehicle recipients displayed complete resolution of ocular inflammation and ocular pain at day 8 post cataract surgery. Complete resolution of pain was seen as early as post-operative day 3. Treatment-related ocular adverse events in the loteprednol etabonate gel 0.38% group occurred in < 1% of subjects and included one incidence each of photophobia, cystoid macular oedema, eyelid oedema and instillation site pain. Treatment with loteprednol etabonate gel 0.38% had no meaningful impact on intraocular pressure (IOP) or visual acuity. Thus, loteprednol etabonate gel 0.38% extends the treatment options available in resolving post-operative inflammation and pain in patients who have undergone ocular surgery.

Dose Uniformity of Loteprednol Etabonate (Submicron) Ophthalmic Gel 0.38% Compared with Prednisolone Acetate Ophthalmic Suspension 1%

“…Both the LE gel 0.5% and LE SM gel 0.38% formulations have similar rheological properties with nearly identical shear-thinning behavior and decreased viscosity on dilution with saline; however, the LE SM gel 0.38% formulation has a reduced drug particle size (an approximately five- to tenfold reduction in diameter), which results in improved drug dissolution, leading to enhanced ocular penetration and bioavailability in the anterior segment tissues most relevant to postsurgery inflammation [ 6 , 7 ]. The reduced particle size in the LE SM gel 0.38% formulation allows for reductions in the active drug concentration and dosing frequency compared with the LE gel 0.5% formulation (three times daily vs. four times daily, respectively) [ 7 ]. Although particle size is reduced in the LE SM gel 0.38% relative to the LE gel 0.5%, both formulations have similar nonsettling properties [ 7 ].…”

“…The reduced particle size in the LE SM gel 0.38% formulation allows for reductions in the active drug concentration and dosing frequency compared with the LE gel 0.5% formulation (three times daily vs. four times daily, respectively) [ 7 ]. Although particle size is reduced in the LE SM gel 0.38% relative to the LE gel 0.5%, both formulations have similar nonsettling properties [ 7 ]. Furthermore, modifications made to the excipients in the LE SM gel 0.38% formulation to stabilize the drug particles (e.g., hypromellose) [ 1 , 6 ] do not appear to affect the nonsettling characteristics of this formulation.…”

“…Most topical ocular corticosteroid formulations (including prednisolone acetate 1% suspension and LE gel 0.5%) require frequent (four times daily) dosing to achieve therapeutic levels of the active drug [ 1 , 8 , 11 ]. LE SM gel 0.38% allows for less frequent (three times daily) administration and, due to its nonsettling properties, requires only one shake (to load the dropper tip); thus, it is expected to improve patient convenience and potentially increase adherence [ 7 ].…”

“…Loteprednol etabonate (submicron) ophthalmic gel 0.38% (LE SM gel 0.38%; Lotemax ® SM; Bausch + Lomb, Rochester, NY, USA), a next-generation corticosteroid formulation with reduced drug particle size and improved ocular penetration compared with loteprednol etabonate ophthalmic gel 0.5% (LE gel 0.5%; Lotemax ® ; Bausch + Lomb, Rochester, NY, USA), is indicated for the treatment of inflammation and pain following ocular surgery [ 1 , 5 – 7 ]. The reduced drug particle size of LE SM gel 0.38% compared with LE gel 0.5% improves ocular penetration and enables a reduction in drug concentration and dosing frequency [ 1 , 6 ].…”

Anti-inflammatory medication use after cataract surgery: An online survey of practice patterns

“…The literature does not clearly establish an optimal AIM regimen, dosing, or duration of treatment. [1][2][3][4][5][6][7][8] Some ophthalmologists prescribe either corticosteroids or NSAIDs as topical monotherapy; others prescribe both in combination, potentially as a result of the ESCRS randomized clinical trial that showed that patients treated with combination therapy had a reduced likelihood of developing clinically significant cystoid macular edema compared with those receiving topical monotherapy. 9 More recently, alternate routes of corticosteroid administration have been tried and adopted in an effort to reduce the need or frequency of topical AIM.…”