Efficient Penetration

Designed to adhere to the ocular surface and then penetrate key ocular tissues1,2

Clinical significance of these preclinical data has not been established.

Formulated with stabilizing ingredients6-10

Poloxamer 407 and hypromellose help stabilize submicron particles, increasing contact with tears7-10

1. Adherence

Similar to LOTEMAX® GEL, polycarbophil helps enhance widespread coverage and prolong exposure on the ocular surface to maximize absorption potential2

2. Rapid DISSOLUTION

Submicron particles have more surface area exposed to tears, driving rapid drug dissolution. In an in vitro assay, ~80% of maximum dissolved loteprednol etabonate was attained at 30 sec3-5

3. Penetration

LOTEMAX® SM efficiently penetrates, with ~2x greater penetration to the aqueous humor than LOTEMAX® GEL (loteprednol etabonate ophthalmic gel) 0.5%2

 OCULAR PENETRATION

Designed to improve drug exposure in key ocular
tissues, without increasing BAK1,5,6,11*

Cmax=Peak drug concentration      AUC(0-24)=Drug exposure over 24 hours

~2x GREATER PENETRATION
to the aqueous humor than LOTEMAX® GEL1

Clinical significance of these preclinical data has not been established.
*Compared to LOTEMAX® GEL.

Study Design: Preclinical study in 108 rabbits to examine the effect of submicron particle size on ocular tissue penetration and drug exposure. Ocular tissues included the conjunctiva, cornea, aqueous humor, and iris/ciliary body.

INDICATION

LOTEMAX® SM (loteprednol etabonate ophthalmic gel) 0.38% is a corticosteroid indicated for the treatment of post-operative inflammation and pain following ocular surgery.

IMPORTANT SAFETY INFORMATION
  • LOTEMAX® SM, as with other ophthalmic corticosteroids, is contraindicated in most viral diseases of the cornea and conjunctiva including epithelial herpes simplex keratitis (dendritic keratitis), vaccinia, and varicella, and also in mycobacterial infection of the eye and fungal diseases of ocular structures.
  • Prolonged use of corticosteroids may result in glaucoma with damage to the optic nerve, defects in visual acuity and fields of vision. If LOTEMAX® SM is used for 10 days or longer, IOP should be monitored.
  • Use of corticosteroids may result in posterior subcapsular cataract formation.
  • The use of steroids after cataract surgery may delay healing and increase the incidence of bleb formation. In those with diseases causing thinning of the cornea or sclera, perforations have been known to occur with the use of topical steroids. The initial prescription and renewal of the medication order should be made by a physician only after examination of the patient with the aid of magnification such as slit lamp biomicroscopy and, where appropriate, fluorescein staining.
  • Prolonged use of corticosteroids may suppress the host response and thus increase the hazard of secondary ocular infections. In acute purulent conditions, steroids may mask infection or enhance existing infections.
  • Employment of a corticosteroid medication in the treatment of patients with a history of herpes simplex requires great caution. Use of ocular steroids may prolong the course and may exacerbate the severity of many viral infections of the eye (including herpes simplex).
  • Fungal infections of the cornea are particularly prone to develop coincidentally with long-term local steroid application. Fungus invasion must be considered in any persistent corneal ulceration where a steroid has been used or is in use. Fungal cultures should be taken when appropriate.
  • Contact lenses should not be worn when the eyes are inflamed.
  • There were no treatment-emergent adverse drug reactions that occurred in more than 1% of subjects in the three times daily group compared to vehicle.

You are encouraged to report negative side effects of prescription drugs to the FDA. Visit www.fda.gov/medwatch or call 1-800-FDA-1088.

Click here for full Prescribing Information for LOTEMAX® SM.

References: 1. Cavet ME, Glogowski S, DiSalvo C, Richardson ME. Ocular pharmacokinetics of submicron loteprednol etabonate ophthalmic gel 0.38% following topical administration in rabbits. Poster presented at 2015 ARVO Annual Meeting; May 4, 2015; Denver, Colorado. 2. Coffey MJ, DeCory HH, Lane SS. Development of a non-settling gel formulation of 0.5% loteprednol etabonate for anti-inflammatory use as an ophthalmic drop. Clin Ophthalmol. 2013;7:299-312. 3. Khadka P, Ro J, Kim H, et al. Pharmaceutical particle technologies: an approach to improve drug solubility, dissolution and bioavailability. Asian J Pharm Sci. 2014;9(6):304-316. 4. Phillips E, Coffey MJ, Shawer M. Viscoelastic and dissolution characterization of submicron loteprednol etabonate ophthalmic gel, 0.38%. Poster presented at 2015 ARVO Annual Meeting; May 4, 2015; Denver, Colorado. 5. Data on file. Bausch & Lomb, Inc. 6. LOTEMAX SM [prescribing information]. Bridgewater, NJ: Bausch & Lomb, Inc. 7. Moghimi SM, Hunter AC. Poloxamers and poloxamines in nanoparticle engineering and experimental medicine. Trends Biotechnol. 2000;18(10):412-420. 8. Giuliano E, Paolino D, Fresta M, Cosco D. Mucosal applications of poloxamer 407-based hydrogels: an overview. Pharmaceutics. 2018;10(3):e159. 9. Shawer M, Phillips E, Coffey MJ, inventors; Bausch & Lomb Incorporated, assignee. Ophthalmic Suspension Composition. US Patent 2016021.3609A1. July 28, 2016. 10. Bhakay A, Rahman M, Dave RN, Bigili E. Bioavailability enhancement of poorly water-soluble drugs via nanocomposites: formulation–processing aspects and challenges. Pharmaceutics. 2018;10(3). pii: E86. 11. LOTEMAX GEL [prescribing information]. Bridgewater, NJ: Bausch & Lomb, Inc.