A novel eye drop of alpha tocopherol to prevent ocular oxidant damage: improve the stability and ocular efficacy

Abstract

The aim of this study was to design novel mixed micelles as an ophthalmic delivery system for alpha-tocopherol (TOC) to prevent its degradation and improve ocular efficacy. The nonionic polymers, Polyoxyl 15 Hydroxystearate (Solutol® HS15) and Pluronic® F127, were discovered to be the most effective agents for retaining the activity and solubilization of TOC, respectively. Prepared by a thin-film hydration method, HS15/Pluronic® F127 yielded good encapsulation percentages of TOC, with a 27.7% drug loading efficiency. Incorporation of cetalkonium chloride (CKC) into HS15/Pluronic® F127 mixed micelles made the zeta potential of the micelles +17 mV, potentially prolonging the residence time of formulations on ocular surfaces. The optimized micelle preparation remained stable when diluted in a synthetic tear solution. It is known that the antioxidant ability of TOC in typical formulations reduces to around 85% of its initial value after 1 month when stored at 4 or 25 °C under an air atmosphere, which limits ophthalmic applications to less than 1 month. However, encapsulated TOC in investigated micelles remained stable for at least 6 months when sealed with N2. Finally, the cationic micelles were well tolerated after multiple administrations in rabbits, and they improved ocular accumulation of TOC. Taken together, these data suggest that the optimized micelle preparations described in this study may be suitable drug carriers for the treatment of ocular oxidant damage.

Topical 1% cyclosporine eyedrops for the treatment of crystalline corneal dystrophy in dogs

“…In previous studies, our research group has shown that a combination of CsA and vitamin E was a safe and effective treatment for keratoconjunctivitis sicca and chronic superficial keratitis in dogs ( Arteaga et al ., 2021 ). Ophthalmic α -tocopherol (TOC) is the most effective antioxidant of the vitamin E family and is receiving special attention to prevent and treat retinopathies, cataracts, and DES, among other ocular pathologies ( Xin et al , 2016 ). In our study, 100% TOC was used as a new solvent of CsA.…”

Fabrication of α-mangostin – loaded liposomes for cytotoxic-activity against A549 lung-cancer spheroids

“…For Alzheimer's patients, high cholesterol levels in the blood may hasten the development of beta-amyloid plaques, the clumpy protein deposits that harm to the brain [20]. Therefore, recent studies have been utilized tocopherol (Toc) to enhance liposome stability [21,22]. Since it is not hazardous to the body at any volume, tocopherols give hopefulness for the potential to improve liposome quality [23].…”

Vitamin E as a Safe and Effective Vehicle for 1% Cyclosporine Eye Drops to Treat Chronic Non-Ulcerative Keratopathies in Dogs and Cats

“…In addition, vitamin E is considered the most important antioxidant present in the body because of its activity against the damaging effects of reactive oxygen species (Mustacich et al 2007;Pekmezci 2011;Peh et al 2016;Miyazawa et al 2019). These properties have fostered the use, in humans, of vitamin E to treat ocular diseases, such as age-related macular degeneration, cataract, uveitis (Xin et al 2016), and to prevent keratocyte apoptosis after refractive surgery (Bilgihan et al 2001). Besides, vitamin E has been shown to protect against UV radiation-induced cataract in albino rat animal models (Ayala and Söderberg 2004).…”