Sustained-release fluocinolone acetonide intravitreal insert for macular edema: clinical pharmacology and safety evaluation

Abstract

The FAc, Retisert is a sustained-release device that is surgically implanted in the vitreous and has been approved by the US FDA for the treatment of non-infectious intermediate, posterior or panuveitis. FAi was developed after FAc and is an intravitreal corticosteroid delivery system that allows controlled release of therapeutic levels of fluocinolone acetonide (FA). Initial efficacy and safety data suggest that this delivery system maintains clinical effectiveness for up to 3 years after a single delivery of the device. This second-generation fluocinolone delivery device has shown superior safety results in clinical trials compared to the previous version of the higher dose FAc (0.59 mg). Sustained delivery preparations may help to reduce the treatment burden and its associated risks by decreasing the frequency of intravitreal injections. However, much needs to be learnt from additional clinical trials, post-marketing surveillance and results of extension studies. Concerns of intravitreal corticosteroids, such as cataract and increase in intraocular pressure, remain major challenges for this therapeutic strategy.

Solid Lipid Nanoparticles Improve the Diclofenac Availability in Vitreous after Intraocular Injection

“…In order to increase the drug residence time in vitreous, application of colloidal carrier system has been evaluated in previous studies [ 13 – 15 ]. Different drug carriers such as liposomes [ 16 ], microspheres [ 17 ], thermogel [ 18 ], and insert [ 19 ] have been used. For example, Abrishami and his colleagues [ 16 ] have evaluated in vitro and in vivo characteristics of bevacizumab nanoliposomes.…”

Novel Therapies in Development for Diabetic Macular Edema

“…It has been recently approved by the US Food and Drug Administration (US-FDA) for the treatment of DME in patients who have previously been treated with corticosteroids and have not experienced a significant rise in intraocular pressure [22]. In the pivotal phase III studies, Fluocinolone Acetonide in diabetic Macular Edema (FAME A and B), employing Iluvien implant, a significantly higher proportion of patients receiving the implant demonstrated ≥15 letter gain compared to those receiving sham injection at month 36 (34 versus 13.4 %) [23••].…”