Safety and Tolerability of Topical Ophthalmic Triamcinolone Acetonide-loaded Liposomes Formulation and Evaluation of Its Biologic Activity in Patients with Diabetic Macular Edema

Abstract

Intravitreal injections (IVTs) of corticosteroids as triamcinolone acetonide (TA) are frequently used for the treatment of many vitreous and retinal disorders. However, IVTs are related to severe ocular complications. Lately, a topical ophthalmic TA loaded liposomes formulation (TALF) was designed to transport TA into the posterior segment of the eye when instilled in the ocular surface. To evaluate the safety, tolerability, and biologic activity of TALF, an animal study and a phase I clinical assay was performed. Moreover, four patients with diabetic macular edema (DME) were treated with TALF in order to explore the biologic activity of the formulation. No inflammation, lens opacity, swelling or intraocular pressure rising were recorded after the instillation of TALF in any of the animal or clinical study. Mainly, mild and transient adverse events such as dry eye (30%) and burning (30%) were reported. TALF improves significantly visual acuity and diminishes central foveal thickness in patients with DME. The current data demonstrate the safety, tolerability, and biologic activity of TALF. It seems that TALF can be used topically to treat vitreous and retinal diseases that respond to TA such as DME, avoiding the use of corticosteroids IVTs and its associated hazards.

Topical Triamcinolone Acetonide-Loaded Liposomes Formulation Used as an Adjuvant to Intravitreal Ranibizumab Therapy for Neovascular Age Related Macular Degeneration

“…Recently, a triamcinolone acetonide-loaded liposome formulation (TALF) was designed to be used topically to release triamcinolone acetonide (TA), a well-known synthetic corticosteroid, into the vitreous cavity and to reach the retinal tissue. The safety, tolerability and efficacy of this novel liposomal formulation was successfully tested in rabbits [35], while its therapeutic activity was clearly verified in patients with refractory pseudophakic cystoid macular edema, diabetic macular edema and macular edema secondary to branch retinal vein occlusion [36][37][38]. TALF demonstrated to enable continuous, controlled, and effective release of triamcinolone acetonide into the posterior segment tissues and was also well tolerated without presenting adverse events such as ocular hypertension or cataract progression [36,38].…”

19F Solid‐State NMR and Vibrational Raman Characterization of Corticosteroid Drug‐Lipid Membrane Interactions

“…Intravitreal injection of drug‐loaded liposomes has been shown to significantly increase the available concentrations and therapeutic half‐life of drugs in the eye [6] . For example, corticosteroids drugs for treatment of edema, inflammation and angiogenic eye diseases have been delivered to the eye with nanostructured lipid carriers [7] …”

“… [6] For example, corticosteroids drugs for treatment of edema, inflammation and angiogenic eye diseases have been delivered to the eye with nanostructured lipid carriers. [7] …”