Penetration of topical and subconjunctival corticosteroids into human aqueous humour and its therapeutic significance

Abstract

Topical and subconjunctival corticosteroids are some of the most effective and compelling treatment options in ocular inflammatory diseases. A systematic review of literature indexed by Ovid MEDLINE & EMBASE was performed up to December 2008. There are few studies on their aqueous penetration in human subjects. This review article discusses the penetration of different ocular corticosteroids into human aqueous humour along with the therapeutic implications on management of ocular surface diseases, immune-related corneal diseases, anterior uveitis and postoperative anti-inflammatory use. In the context of the paucity of well-constructed, prospective clinical trials comparing the efficacy of different corticosteroids, it provides guiding principles for the use of topical corticosteroids. Dexamethasone alcohol 0.1% and prednisolone acetate 1% are potent corticosteroids, but the latter achieves the highest aqueous concentration within 2 h and maintains higher levels for 24 h. Subconjunctival corticosteroids provide very high concentrations in the aqueous which maintain higher concentrations for longer periods

Optimization of Subconjunctival Biodegradable Microfilms for Sustained Drug Delivery to the Anterior Segment in a Small Animal Model

“…[33][34][35][36] Moreover, the acetate analogue of prednisolone is more hydrophobic; hence, it has a higher tendency to stay attached to the PLC microfilms rather than be released within a short period of time. Therefore, we chose PA as the loading drug in our study.…”

Efficacy and safety comparison of topical loteprednol and topical non-steroidal anti-inflammatory drugs in seasonal allergic conjunctivitis: a prospective open label comparative study

“…Loteprednol, the soft steroid may be preferable to the conventional topical steroids in allergic ocular inflammation as it is rapidly hydrolyzed to its inactive metabolites in the corneal and intraocular tissues and hence free from various steroid related ocular complications. 4,[16][17][18][19] …”

Ocular Pharmacokinetics of Mapracorat, a Novel, Selective Glucocorticoid Receptor Agonist, in Rabbits and Monkeys

“…However, somewhat higher mapracorat concentrations in aqueous humor were observed at doses Ͼ50 g/eye, suggesting that distribution of mapracorat into aqueous humor may be partly limited by preferential distribution into surrounding tissues with a finite capacity that is saturated at doses greater than 50 g/eye. Drug levels in aqueous humor are occasionally used for topical ophthalmic therapeutic agents as a surrogate marker for ocular penetration and/or pharmacologic efficacy (McCulley et al, 2006;Awan et al, 2009). However, the present investigation illustrates an exception to this practice, because aqueous humor levels of mapracorat accurately reflect neither the pharmacokinetics in the surrounding tissue nor apparently its pharmacodynamic effects.…”