Topical Dexamethasone-Cyclodextrin Microparticle Eye Drops for Diabetic Macular Edema

Abstract

Based on this short pilot study, topical dexamethasone-cyclodextrin eye drops are well tolerated, decrease central macular thickness, and improve visual acuity in DME. The results encourage comparative studies between dexamethasone cyclodextrin microparticle eye drops and other treatments for DME. (http://www.umin.ac.jp/ctr number, UMIN000001790.).

Corneal permeation properties of a charged lipid nanoparticle carrier containing dexamethasone

“…Although these methods can achieve high drug concentrations in the posterior segment of the vitreous humor, lens, retina, and other ocular tissues, their broad clinical application is limited by potential complications such as tissue damage, infection and injury, and retinal hemorrhage. [8][9][10][11] Drug administration into the anterior segment has been proposed to circumvent these problems. In intraocular administration, drug molecules must diffuse over a long distance from the site of corneal penetration and penetrate the ocular barrier -which consists of the convection flow of the aqueous humor from the ciliary body to Schlemm's canal, together with lacrimal fluid, blood-aqueous humor, retinal blood, and a corneal avascular component -and be specifically absorbed by the retinal pigment epithelium.…”

“…14,15 Cyclodextrin has been widely studied as a carrier in ophthalmic drug delivery systems and has been shown to prolong ocular retention time and increase drug solubility and bioavailability, thereby improving the drug's effectiveness. 11,16,17 Eye drops consisting of methazolamide in cyclodextrin can also reduce intraocular pressure, and are released over 6 h. The combination of acetazolamide, cyclodextrin, and triethanolamine was shown to increase permeation through the rabbit cornea by over ten-fold and to reduce intraocular pressure by .30%. 18 For diseases requiring long-term drug administration such as those of the retina and vitreous body, a dexamethasone/cyclodextrin mixture applied to the ocular surface increased retinal penetration two-fold relative to systemic administration.…”

Topical dexamethasone–cyclodextrin microparticle eye drops for uveitic macular oedema

“…Topical steroid generally is of little benefit for the treatment of posterior segment diseases. Dexamethasone eye drops containing c-cyclodextrin-based nanoparticles, however, have recently been shown to be effectively delivered to the posterior part of the eye to treat diabetic CME (Loftsson & Stef ansson 2002;Loftsson et al 2007;Tanito et al 2011). Therefore, it seems tempting to examine the effect of this dexamethasone eye drop formulation for the treatment of uveitis with posterior manifestations.…”

Novel Therapies in Development for Diabetic Macular Edema

“…A pilot clinical trial including 19 patients with DME has tested the safety and efficacy of topical dexamethasone-cyclodextrin 1.5 % topical formulation. The results of the study are encouraging and further research is needed to establish the role of these drug delivery systems [26].…”