Pharmacology of Corticosteroids for Diabetic Macular Edema

Abstract

PurposeCorticosteroids remain the mainstay of treatment for inflammatory diseases almost 80 years after their first clinical use. Topical ophthalmic formulations of corticosteroids have been available to treat disease of the anterior segment of the eye, but the approval of corticosteroids to treat vitreoretinal diseases, including vein occlusion, diabetic macular edema, and uveitis, has occurred only recently. Although most diseases respond to corticosteroid therapy, some patients are resistant to this therapy and side effects, including cataract and elevated intraocular pressure, can limit their use. The purpose of this review is to detail the basic science of corticosteroids focusing on differences in potency, drug delivery, pharmacokinetics, and gene activation, and how these differences affect safety and efficacy in the treatment of diabetic macular edema.MethodsA review was conducted of basic science and pharmacology of the corticosteroids used to treat diabetic macular edema.ResultsClinically available corticosteroids not only have differing potency and pharmacokinetics, but also activate different genes in different target tissues. These differences are associated with distinct efficacy, pharmacokinetic, and safety profiles. It is important to understand these differences in selecting corticosteroids to treat diabetic macular edema.ConclusionsRecent advances in our understanding of the basic science of corticosteroids can explain clinical differences in these agents regarding efficacy and safety. Importantly, this understanding should allow the future discovery of additional novel corticosteroids to treat diabetic macular edema.

Recent advances in slow and sustained drug release for retina drug delivery

“…Retinal diseases remain the main causes of visual impairment in industrialized countries due to population aging and to the high prevalence of diabetes and of myopia [1,2]. Major therapeutic advances have been achieved in the last 15 years in the field of retinal diseases allowing not only to stabilize vision of patients presenting macular edema of various origins including diabetic retinopathy, choroidal neovascularization secondary to age-related macular degeneration or to myopia, and to retinal vein occlusion, but also to reach clinically significant vision gain using repeated intraocular administration of either anti-angiogenic recombinant proteins [3][4][5][6] or different glucocorticoids formulations [7][8][9]. These therapies reduce macular edema [10] but they do not cure the disease explaining that the symptoms recur when the drug reaches the lowest efficacy threshold.…”

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“…They are also commonly prescribed to prevent organ transplant rejection and to treat cancers of the lymphoid system such as leukemias, lymphomas, and myelomas (7,8). However, patients chronically treated with synthetic glucocorticoids are prone to severe side effects including osteoporosis, diabetes, obesity, glaucoma, growth retardation in children, and hypertension among others (9)(10)(11).…”

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“…Currently, the therapeutic approaches of DR mainly include surgery, laser photocoagulation, hormone, and anti-vascular endothelial growth factor (VEGF) drug. However, the current treatment could bring some adverse reactions, such as high intraocular pressure, angiogenesis, retinal hemorrhage, and so on [4,5]. Therefore, it is urgent to discover promising therapeutic targets and develop new therapeutic strategies for DR patients.…”