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利用基于商用硅酮的软性隐形眼镜中的维生素E扩散屏障实现环丙沙星的长效释放。

Extended Ciprofloxacin Release Using Vitamin E Diffusion Barrier From Commercial Silicone-Based Soft Contact Lenses.

作者信息

Shayani Rad Maryam, Mohajeri Seyed Ahmad

机构信息

Student Research Committee (SRC) (M.S.R.), Mashhad University of Medical Sciences, Mashhad, Iran; and Pharmaceutical Research Center (M.S.R., S.A.M.), School of Pharmacy, Mashhad University of Medical Sciences, Mashhad, Iran.

出版信息

Eye Contact Lens. 2017 Mar;43(2):103-109. doi: 10.1097/ICL.0000000000000245.

Abstract

OBJECTIVES

Ciprofloxacin (Cipro) is an antibiotic, widely used in form of ophthalmic drops (0.3%) for the treatment of eye infections. In this study, vitamin E was used as a hydrophobic barrier to improve and prolong the amount and time of Cipro release from silicone-based soft contact lenses.

METHODS

Three different commercial contact lenses (Air Optix, Biofinity, and Acuvue Oasys) were soaked in vitamin E solutions (0.1 and 0.2 g/mL). The effect of vitamin E on Cipro loading amount and drug releasing profile was evaluated in artificial tear. Swelling properties and diameter changes of the lenses were also investigated in aqueous media in presence and absence of vitamin E.

RESULTS

The data indicated that vitamin E, as a hydrophobic barrier, significantly decreased the water content of silicone-based soft contact lenses. After vitamin E loading, a 5% to 18% increase was observed in lens diameter in the hydrated state, whereas the lens diameter increased by 11% to 23% in the dry state. In all commercial lenses, vitamin E loading in a 0.2-g/mL solution caused a 27.94% to 37.08% increase in Cipro binding. The results indicated that applying vitamin E loading solutions, with 0.1 and 0.2 g/mL concentrations, could effectively enhance Cipro release time from 2 hr (in a pure non-vitamin E-loaded lens) to 14 to 17 and 30 to 33 days, respectively. These values showed an increase by a factor of 168 to 204 and 360 to 396 in Cipro release time after using vitamin E loading solutions with 0.1 and 0.2 g/mL concentrations, respectively, compared with pure non-vitamin E-loaded soft contact lenses.

CONCLUSIONS

This study indicated that vitamin E acts as an effective hydrophobic barrier, in increasing the Cipro loading capacity of silicone-based contact lenses and prolonging the drug release into the artificial tear.

摘要

目的

环丙沙星(西普乐)是一种抗生素,广泛以0.3%眼药水的形式用于治疗眼部感染。在本研究中,维生素E被用作疏水屏障,以改善和延长环丙沙星从硅基软性隐形眼镜中的释放量和释放时间。

方法

将三种不同的商用隐形眼镜(爱尔康水润舒适氧、博士伦纯视2代、强生欧舒适)浸泡在维生素E溶液(0.1和0.2 g/mL)中。在人工泪液中评估维生素E对环丙沙星负载量和药物释放曲线的影响。还在有无维生素E的水性介质中研究了镜片的溶胀特性和直径变化。

结果

数据表明,维生素E作为疏水屏障,显著降低了硅基软性隐形眼镜的含水量。负载维生素E后,水合状态下镜片直径增加了5%至18%,而干燥状态下镜片直径增加了11%至23%。在所有商用镜片中,以0.2 g/mL溶液负载维生素E使环丙沙星结合量增加了27.94%至37.08%。结果表明,应用浓度为0.1和0.2 g/mL的维生素E负载溶液可有效将环丙沙星的释放时间从2小时(在未负载维生素E的纯镜片中)分别延长至14至17天和30至33天。与未负载维生素E的纯软性隐形眼镜相比,使用浓度为0.1和0.2 g/mL的维生素E负载溶液后,这些值显示环丙沙星释放时间分别增加了168至204倍和360至396倍。

结论

本研究表明,维生素E作为有效的疏水屏障,可提高硅基隐形眼镜的环丙沙星负载能力,并延长药物向人工泪液中的释放时间。

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