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

Drug Development and Industrial Pharmacy
Jiayu XinHongzhuo Liu

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 admini...Continue Reading

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Citations

Apr 21, 2020·Journal of Ocular Pharmacology and Therapeutics : the Official Journal of the Association for Ocular Pharmacology and Therapeutics·Meltem Ezgi DurgunYıldız Özsoy
Dec 25, 2019·International Journal of Pharmaceutics·Maria Aurora GrimaudoGiovanni Puglisi
Jul 31, 2020·Expert Opinion on Drug Metabolism & Toxicology·Vrinda GoteDhananjay Pal

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