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Pharmaceutical technology can turn a traditional drug, dexamethasone into a first-line ocular medicine. A global perspective and future trends

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Abstract

Dexamethasone is one of the most prescribed glucocorticoids. It is effective and safe in the treatment of a wide variety of ocular conditions, including anterior and posterior segment inflammation. However, its half-life in the vitreous humor is very short, which means that it typically requires frequent administrations, thus reducing patient adherence and causing therapeutic failure. Innovative dexamethasone delivery systems have been designed in an attempt to achieve sustained release and targeting. The FDA has approved dexamethasone implants for the treatment of macular edema secondary to retinal vein occlusion and posterior segment noninfectious uveitis. Lenses, micro- and nanoparticles, liposomes, micelles and dendrimers are also proving to be adequate systems for maintaining optimal dexamethasone levels in the site of action. Pharmaceutical technology is turning a classical drug, dexamethasone, into a fashionable medicine.

Section snippets

Dexamethasone and ocular diseases

Among all the corticosteroids available for the treatment of ocular diseases, dexamethasone (Fig. 1, 9-Fluoro-11,17,21-trihydroxy-16-methylpregna-1,4-diene-3,20-dione) is one of the most prescribed worldwide (Rodriguez Villanueva et al., 2016a). It is used to treat a wide variety of ocular conditions, including diseases of both anterior segment inflammation (such as keratitis, blepharitis, allergic conjunctivitis, anterior uveitis and dry eye) and, recently, posterior segment inflammation (such

Dexamethasone pharmaceutical systems designed to treat anterior segment of the eye diseases

Challenges in the design of new systems to treat diseases affecting the anterior segment of the eye include increasing precorneal retention and corneal permeability. A multitude of attempts have been made to handle these challenges using conventional forms of dosage. One of the proposed strategies consists of modifying the mucoadhesivity of hydrogels. To achieve this, Kesavan et al. (2011) included tensioactives (Carbopol 980NF and NaCMC at 0.2% m/w and 0.4% m/w, respectively, for optimum

Systems designed for topical administration

Recently, some attempts have been made regarding retinal delivery of lipophilic drugs after topical administration using mixed nanomicelles. Mixed nanomicelles enhance the solubility of drugs and increase their penetration across the conjunctival epithelium, presumably by temporarily altering the tight junctions (Vadlapudi and Mitra, 2013). Nanomicelles formulated with dexamethasone and with a 7:3 ratio of polyoxyl 40 stearate and polysorbate 80 (2 amphiphilic surfactants approved by the FDA

An overview

Dexamethasone is one of the most commonly prescribed glucocorticoids. For ocular therapeutic uses, despite the controversy regarding the initial phases, dexamethasone can be stated to be effective and safe in a wide variety of ocular diseases. Furthermore, it is full of possibilities. In addition to the enormously popular anti-inflammatory effect, a novel pharmacological mechanism for the observed ocular neuroprotective activity has been proposed (Calvo et al., 2015). New developments in

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