Loteprednol etabonate in ophthalmic practice: clinical and pharmacological aspects of use
DOI: 10.32364/2311-7729-2026-26-3-9
Loteprednol etabonate in ophthalmic practice: clinical and pharmacological aspects of use
G.Yu. Knorring
Russian University of Medicine, Moscow, Russian Federation
Anti-inflammatory agents are an important component of the treatment of inflammatory eye diseases and are also used in other clinical settings, including the postoperative period in ophthalmic surgery. The most commonly used anti-inflammatory agents in ophthalmic practice are glucocorticosteroids (GCS) and nonsteroidal anti-inflammatory drugs. Loteprednol etabonate (LE) is a topical GCS developed for ophthalmic use. Its distinctive chemical structure, including the presence of an ester group, places LE among the so-called "soft steroids": following exertion of its pharmacological effect, the molecule undergoes metabolism to inactive metabolites. This article reviews the clinical and pharmacological characteristics of LE, including its lipophilicity, penetration into ocular tissues, affinity for glucocorticoid receptors, anti-inflammatory activity, and effects on intraocular pressure. Particular attention is given to comparisons of LE with other topical GCS used in ophthalmology, as well as to available data on its effects on the ocular surface and safety profile. The available evidence supports the consideration of LE as an option for topical anti-inflammatory therapy in diseases and conditions associated with inflammation of the anterior segment of the eye, taking into account its pharmacological features and tolerability.
Keywords: topical glucocorticosteroids, loteprednol etabonate, uveitis, epitheliopathy, dexamethasone.
For citation: Knorring G.Yu. Loteprednol etabonate in ophthalmic practice: clinical and pharmacological aspects of use. Russian Journal of Clinical Ophthalmology. 2026;26(3):255–261 (in Russ.). DOI: 10.32364/2311-7729-2026-26-3-9
About the author:
German Yu. Knorring — C. Sc. (Med.), Associate Professor of the Department of Therapy, Clinical Pharmacology and Emergency Medical Care, Faculty of General Medicine, N.A. Semashko Research and Educational Institute of Clinical Medicine, Russian University of Medicine; 4, Dolgorukovskaya str., Moscow, 127006, Russian Federation; ORCID iD 0000-0003-4391-2889
Contact information: German Yu. Knorring, e-mail: knorring@mail.ru
Financial Disclosure: the author has no financial or property interest in any material or method mentioned.
There is no conflict of interest.
Received 02.06.2026.
Revised 24.06.2026.
Accepted 20.07.2026.
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2. Зырянов С.К., Бутранова О.И. Топические глюкокортикостероиды в офтальмологии: сравнительный анализ эффективности и безопасности. Российский офтальмологический журнал. 2023;16(2):166–172. DOI: 10.21516/2072-0076-2023-16-2-166-172. Zyryanov S.K., Butranova O.I. Topical glucocorticoids in ophthalmology: a comparative analysis of efficacy and safety. Russian Ophthalmological Journal. 2023;16(2):166–172 (in Russ.). DOI: 10.21516/2072-0076-2023-16-2-166-172
3. Khoo P., Cabrera-Aguas M., Watson S.L. Topical steroids as adjunctive therapy for bacterial keratitis: Evidence from a retrospective case series of 313 cases. Asia Pac J Ophthalmol (Phila). 2020;9(5):398–403. DOI: 10.1097/APO.0000000000000320
4. Lin A., Rhee M.K., Akpek E.K. et al. Bacterial keratitis preferred practice pattern®. Ophthalmology. 2019;126(1):1–55. DOI: 10.1016/j.ophtha.2018.10.018
5. Ghadiri N., Reekie I.R., Gordon I. et al. Systematic review of clinical practice guidelines for uveitis. BMJ Open Ophthalmology. 2023;8:e001091. DOI: 10.1136/bmjophth-2022-001091
6. Офтальмология: национальное руководство. Под ред. С.Э. Аветисова, Е.А. Егорова, Л.К. Мошетовой и др. 3-е изд., перераб. и доп. М.: ГЭОТАР-Медиа; 2024. Ophthalmology: national guide. S.E. Avetisov, E.A. Egorov, L.K. Moshetova et al., eds. 3rd ed., revised and additional M.: GEOTAR-Media; 2024 (in Russ.).
7. Löwenberg M., Stahn C., Hommes D.W., Buttgereit F. Novel insights into mechanisms of glucocorticoid action and the development of new glucocorticoid receptor ligands. Steroids. 2008;73(9-10):1025–1029. DOI: 10.1016/j.steroids.2007.12.002
8. Майчук Д.Ю., Тарханова А.А. Преимущества «мягких стероидов» в лечении воспалительных заболеваний глаз. Обзор. Офтальмология. 2021;18(4):778–783. Maychuk D.Yu., Tarkhanova A.A. Advantages of "Soft Steroids" in the Treatment of Inflammatory Eye Diseases. Оverview. Ophthalmology in Russia. 2021;18(4):778–783 (in Russ.). DOI: 10.18008/1816-5095-2021-4-778-783
9. Onyimba C.U., Vijapurapu N., Curnow S.J. et al. Characterisation of the prereceptor regulation of glucocorticoids in the anterior segment of the rabbit eye. J Endocrinol. 2006;190(2):483–493. DOI: 10.1677/joe.1.06840
10. Витовская О.П. Медикаментозно индуцированная глаукома. Офтальмологические ведомости. 2014;7(3):58–62. Vitovskaya O.P. Drug-induced glaucoma. Ophthalmological News. 2014;7(3):58–62 (in Russ.).
11. McGhee C.N., Dean S., Danesh-Meyer H. Locally administered ocular corticosteroids: benefits and risks. Drug Saf. 2002;25:33–55. DOI: 10.2165/00002018-200225010-00004
12. Sheppard J.D., Comstock T.L., Cavet M.E. Impact of the Topical Ophthalmic Corticosteroid Loteprednol Etabonate on Intraocular Pressure. Adv Ther. 2016;33(4):532–552. DOI: 10.1007/s12325-016-0315-8
13. Comstock T.L., Decory H.H. Advances in corticosteroid therapy for ocular inflammation: loteprednol etabonate. Int J Inflam. 2012;2012:789623. DOI: 10.1155/2012/789623
14. Alberth M., Wu W.M., Winwood D., Bodor N. Lipophilicity, solubility and permeability of loteprednol etabonate: a novel, soft anti-inflammatory corticosteroid. J Biopharm Sci. 1991;2(2):115–125. DOI: 10.1002/bdd.2510080605
15. Katz M., Gans E.H.. Topical corticosteroids, structure-activity and the glucocorticoid receptor: discovery and development a process of "planned serendipity". J Pharm Sci. 2008;97(8):2936–2947. DOI: 10.1002/jps.21222
16. Schopf L., Enlow E., Popov A. et al. Ocular Pharmacokinetics of a Novel Loteprednol Etabonate 0.4% Ophthalmic Formulation. Ophthalmol Ther. 2014;3(1-2):63–72. DOI: 10.1007/s40123-014-0021-z
17. Sulaiman R.S., Kadmiel M., Cidlowski J.A. Glucocorticoid receptor signaling in the eye. Steroids. 2018;133:60–66. DOI: 10.1016/j.steroids.2017.11.002
18. Druzgala P., Wu W.M., Bodor N. Ocular absorption and distribution of loteprednol etabonate, a soft steroid, in rabbit eyes. Curr Eye Res. 1991;10(10):933–937. DOI: 10.3109/02713689109020329
19. Druzgala P., Hochhaus G., Bodor N. Soft drugs-10. Blanching activity and receptor binding affinity of a new type of glucocorticoid: loteprednol etabonate. J Steroid Biochem Mol Biol. 1991;38(2):149–154. DOI: 10.1016/0960-0760(91)90120-t
20. Samudre S.S., Lattanzio F.A. Jr, Williams P.B., Sheppard J.D.Jr. Comparison of topical steroids for acute anterior uveitis. J Ocul Pharmacol Ther. 2004;20(6):533–547. DOI: 10.1089/jop.2004.20.533
21. Grigorian R.A., Shah A., Guo S. Comparison of loteprednol etabonate 0.5% (Lotemax) to prednisolone acetate 1% (Falcon) for inflammation treatment following cataract surgery [abstract]. Presented at: Association for Research in Vision and Ophthalmology Annual Meeting; Fort Lauderdale, FL; May 6–10, 2007. Abstract 1065/B1040.
22. Lane S.S., Holland E.J. Loteprednol etabonate 0.5% versus prednisolone acetate 1.0% for the treatment of inflammation after cataract surgery. J Cataract Refract Surg. 2013;39(2):168–173. DOI: 10.1016/j.jcrs.2012.10.039
23. Chen Y., Wang X., Gao M. et al. The effect of loteprednol suspension eye drops after corneal transplantation. BMC Ophthalmol. 2021;21(1):234. DOI: 10.1186/s12886-021-01982-8
24. Patel P.D., Kodati B., Clark A.F. Role of Glucocorticoids and Glucocorticoid Receptors in Glaucoma Pathogenesis. Cells. 2023;12:2452. DOI: 10.3390/cells12202452
25. Ших Е.В., Махова А.А. Дифлупреднат: клинико-фармакологический анализ опыта и перспектив применения в фармакотерапии глазных болезней. Клиническая офтальмология. 2025;25(1):42–48. DOI: 10.32364/2311-7729-2025-25-1-6. Shikh E.V., Makhova A.A. Difluprednate: clinical pharmacological analysis of experience and prospects of its application in eye disease pharmacotherapy. Russian Journal of Clinical Ophthalmology. 2025;25(1):42–48 (in Russ.). DOI: 10.32364/2311-7729-2025-25-1-6
26. Naageshwaran V., Ranta V.P., Toropainen E. et al. Topical pharmacokinetics of dexamethasone suspensions in the rabbit eye: Bioavailability comparison. Int J Pharm. 2022;615:121515. DOI: 10.1016/j.ijpharm.2022.121515
27. Kadmiel M., Janoshazi A., Xu X., Cidlowski J.A. Glucocorticoid action in human corneal epithelial cells establishes roles for corticosteroids in wound healing and barrier function of the eye. Exp Eye Res. 2016;152:10–33. DOI: 10.1016/j.exer.2016.08.020
28. Ayaki M., Iwasawa A., Niwano Y. Comparative assessment of the cytotoxicity of six anti-inflammatory eyedrops in four cultured ocular surface cell lines, as determined by cell viability scores. Clin Ophthalmol. 2012;6:1879–1884.
29. Gokhale N.S., Vemuganti G.K. Diclofenac-induced acute corneal melt after collagen crosslinking for keratoconus. Cornea. 2010;29(1):117–119. DOI: 10.1097/ICO.0b013e3181a06c31
30. Кнорринг Г.Ю. Применение декспантенола при повреждении роговицы. Вестник офтальмологии. 2023;139(6):119–124. Knorring G.Yu. Use of dexpanthenol in corneal damage. Russian Annals of Ophthalmology. 2023;139(6):119–124 (in Russ.). DOI: 10.17116/oftalma2023139061119
31. Muzyka-Woźniak M., Stróżecki Ł., Przeździecka-Dołyk J. Assessment of the eye surface and subjective symptoms after using 0.1% dexamethasone drops with and without preservatives in patients after cataract surgery. Sci Rep. 2023;13:18625. DOI: 10.1038/s41598-023-44939-1
32. Sheppard J.D., Donnenfeld E.D., Holland E.J. et al. Effect of loteprednol etabonate 0.5% on initiation of dry eye treatment with topical cyclosporine 0.05%. Eye Contact Lens. 2014;40(5):289–296. doi: 10.1097/ICL.0000000000000049
33. Pflugfelder S.C., Maskin S.L., Anderson B. et al. A randomized, double-masked, placebo-controlled, multicenter comparison of loteprednol etabonate ophthalmic suspension, 0.5%, and placebo for treatment of keratoconjunctivitis sicca in patients with delayed tear clearance. Am J Ophthalmol. 2004;138(3):444–457. DOI: 10.1016/j.ajo.2004.04.052
34. Mazet R., Yaméogo J.B.G., Wouessidjewe D. et al. Recent Advances in the Design of Topical Ophthalmic Delivery Systems in the Treatment of Ocular Surface Inflammation and Their Biopharmaceutical Evaluation. Pharmaceutics. 2020;12(6):570. DOI: 10.3390/pharmaceutics12060570
35. Novack G.D., Howes J., Crockett R.S., Sherwood M.B. Change in intraocular pressure during long-term use of loteprednol etabonate. J Glaucoma. 1998;7:266–269. PMID: 9713785
36. Pleyer U., Ursell P.G., Rama P. Intraocular pressure effects of common topical steroids for post-cataract inflammation: are they all the same? Ophthalmol Ther. 2013;2(2):55–72. DOI: 10.1007/s40123-013-0020-5
37. Price M.O., Feng M.T., Scanameo A., Price F.W.Jr. Loteprednol Etabonate 0.5% Gel Vs. Prednisolone Acetate 1% Solution after descemet membrane endothelial keratoplasty: Prospective randomized trial. Cornea. 2015;34(8):853–858. DOI: 10.1097/ICO.0000000000000475
38. Price M.O., Price F.W. Jr, Kruse F.E. et al. Randomized comparison of topical prednisolone acetate 1% versus fluorometholone 0.1% in the first year after descemet membrane endothelial keratoplasty. Cornea. 2014;33(9):880–886. DOI: 10.1097/ICO.0000000000000206
39. The Loteprednol Etabonate Postoperative Inflammation Study Group 2. A double-masked, placebo-controlled evaluation of 0.5% loteprednol etabonate in the treatment of postoperative inflammation. Ophthalmology. 1998;105:1780–1786. DOI: 10.1016/s0161-6420(98)99054-6
40. Elettreby A.M., Alsaied M.A., Saleh M.M. et al. Efficacy and Safety of Loteprednol Etabonate in Managing Pain and Inflammation After Cataract Surgery: A Systematic Review and Meta-analysis. Eye Contact Lens. 2025;51(11):481–490. DOI: 10.1097/ICL.0000000000001210
41. Koçluk Y., Sukgen E.A., Cevher S., Mat E. Symptomatic Treatment of Subepithelial Infiltrates after Viral Conjunctivitis: Loteprednol or Dexamethasone? Ocul Immunol Inflamm. 2017;25(5):649–653. DOI: 10.3109/09273948.2016.1149593
42. Gill M.S., Murphy D.A., Dvorak J.D. et al. Fill levels, cost comparisons, and expulsion force requirements of commonly used topical ophthalmic steroids. J Cataract Refract Surg. 2022;48(4):475–480. DOI: 10.1097/j.jcrs.0000000000000833
43. Sendrowski D.P. et al. Anti-inflammatory drugs. In: Bartlett J.D., Jaanus S.O., eds. Clinical Ocular Pharmacology. 5th ed. St. Louis: Butterworth-Heinemann; 2008.
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