Abstract
Treatment of uveitis (i.e., inflammation of the uvea) is challenging due to lack of convenient ophthalmic dosage forms. This work is aimed to determine the efficiency of triamcinolone acetonide (TA)-loaded microemulsion as an ophthalmic delivery system for the treatment of uveitis. Water titration method was used to construct different pseudo-ternary phase diagrams. Twelve microemulsion formulations were prepared using oleic acid, Cremophor EL, and propylene glycol. Among all tested formulations, Formulation F3, composed of oil: surfactant-co-surfactant (1:1): water (15:35:50% w/w, respectively), was found to be stable and showed acceptable pH, viscosity, conductivity, droplet size (211 ± 1.4 nm), and zeta potential (−25 ± 1.7 mV) and almost complete in vitro drug release within 24 h. The in vivo performance of the optimized formulation was evaluated in experimentally uveitis-induced rabbit model and compared with a commercial TA suspension (i.e., Kenacort®-A) either topically or by subconjunctival injection. Ocular inflammation was evaluated by clinical examination, white blood cell count, protein content measurement, and histopathological examination. The developed TA-loaded microemulsion showed superior therapeutic efficiency in the treatment of uveitis with high patient compliance compared to commercial suspension. Hence, it could be considered as a potential ocular treatment option in controlling of uveitis.
Highlights
Uveitis is an inflammation in the uveal layer of the eye that lies below the sclera and cornea which includes iris, choroid, and ciliary body
The exceptional high drug solubility in castor oil compared with other vegetable oils can be attributed to the presence of ricinoleic acid which has a hydroxyl functional group that increases castor oil polarity compared to other oils [46]
Based on the microemulsion area, oleic acid, Cremophor EL, and propylene glycol (PG) were chosen as an oil, surfactant, and co-surfactant, respectively
Summary
Uveitis is an inflammation in the uveal layer of the eye that lies below the sclera and cornea which includes iris, choroid, and ciliary body. It may affect retina, vitreous, sclera, and optic nerve. It is associated with about 10% of the blindness cases in the whole world [1]. Most challenges in dealing with uveitis are related to the treatment of the posterior segment inflammation. Corticosteroids (e.g., dexamethasone, triamcinolone acetonide (TA), and fluocinolone acetonide) and immunosuppressant agents are the commonly used agents in the treatment of uveitis [2]
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