Corticosteroids in ophthalmology: drug delivery innovations, pharmacology, clinical applications, and future perspectives

Abstract

Corticosteroids remain the mainstay of the treatment for various ocular conditions affecting the ocular surface, anterior and posterior segments of the eye due to their anti-inflammatory, anti-oedematous and anti-neovascularization properties. Prednisolone, prednisolone acetate, dexamethasone, triamcinolone acetonide, fluocinolone acetonide, and loteprednol etabonate are amongst the most widely used ophthalmic corticosteroids. Corticosteroids differ in their activity and potency in the eye due to their inherent pharmacological and pharmaceutical differences.Different routes and regimens are available for ocular administration of corticosteroids. Conventional topical application to the eye is the route of choice when targeting diseases affecting the ocular surface and anterior segment, while periocular, intravitreal, and suprachoroidal injections can 3 be potentially effective for posterior segment diseases. Corticosteroid-induced intraocular pressure elevation and cataract formation remain the most significant local risks following topical as well as systemic corticosteroid administration. Invasive drug administration via intracameral, subconjunctival and intravitreal injection can enhance ocular bioavailability and minimize dose and dosing frequency of administration, yet may exacerbate ocular side effects of corticosteroids. This review provides a critical appraisal of the ophthalmic uses of corticosteroid, routes of administration, drug delivery fundamentals and novel ocular implantable steroids delivery systems, factors influencing side effects and future perspectives for ocular corticosteroid therapy.

Ocular Drug Delivery to the Retina: Current Innovations and Future Perspectives

“…According to Chen et al, preservative-free TAs have smaller particle size, with uniform distribution, slower dissolution, and lower free drug level in the vitreous, leading to better and longer duration of drug efficacy than preserved TA [70]. These microcrystal TA drug particles form a depot after intravitreal injection, thereby inducing controlled release and long-lasting therapeutic effects [71]. Missel et al suggested that the depot formulation decreases the dissolution rates within the vitreous Recently, a depot formulation of sunitinib malate (GB-102, GrayBug Vision, Redwood City, CA, USA), a tyrosine kinase inhibitor targeting both VEGF-A and platelet-derived growth factor (PDGF), was developed and tested in a human clinical trial.…”

Effect of Poly(L-lysine) and Heparin Coatings on the Surface of Polyester-Based Particles on Prednisolone Release and Biocompatibility

“…The objective of this study was to elucidate the effect of surface properties of polyestersbased micro-and nanoparticles with different hydrophobicities on the release kinetics of the encapsulated model drug prednisolone. This corticosteroid was selected as a model drug for future studies because it was extensively used in treatments of numerous inflammatory eye diseases [4,26,40], either in the form of eye drops or ointment. The in vitro prednisolone release profiles during 720 h (Figure 3A,C) and 6 h (Figure 3B,D) clearly show the effect of both MPs and NP surface modification on the drug dissolution kinetics.…”

“…Nanotechnology is currently attracting attention for improving the treatment of ocular anterior and posterior segments disorders [1][2][3]. Thereby topical, intravitreal, subconjunctival, and systemic administrations appear feasible [4]. Topical treatment is the most convenient route and is most frequently used for conventional formulations in ophthalmology [5,6].…”

Dexamethasone-Loaded Nanostructured Lipid Carriers for the Treatment of Dry Eye Disease

“…While some of the well-known side effects of corticosteroids (cataracts, increased IOP, etc. ), were outlined in a recent review by Gaballa et al, they also outlined the potential to mitigate such effects by localized, low dose administration, and highlighted the continued interest in the ophthalmic treatment potential of these drugs [ 4 ].…”