开发含溴莫尼定iosomes的隐形眼镜,为青光眼治疗提供缓释和前景广阔的给药系统

IF 2.5 4区 医学 Q3 PHARMACOLOGY & PHARMACY
Shresthi Tripathi, Khushwant S. Yadav
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引用次数: 0

摘要

背景眼压升高是青光眼的常见症状。严重时可能导致失明。由于眼部的生理屏障会阻碍药物到达患病部位,因此青光眼的治疗非常困难。传统制剂(眼药水)停留时间短,会迅速通过鼻泪管排出,导致药物不良反应增加,疗效降低。使用纳米颗粒(如niosomes)可以解决这些问题。虽然niosomes能提高药物渗透性,但对药物的眼部滞留影响不大。本研究旨在制备和评估布利莫尼定含药隐形眼镜,用于治疗青光眼。隐形眼镜以不同的时间间隔(3-10 天)浸泡在含盐雾剂配方中。之后,对隐形眼镜的透光率、膨胀率、药物定量和体外药物释放进行了评估。药效学研究的目的是评估白化兔眼压(IOP)的降低情况。研究比较了含溴莫尼定iosomes 的隐形眼镜与市场上销售的iosomes 制剂在降低眼压方面的效果。结果 通过浸泡法,与市场上销售的制剂相比,含溴莫尼定iosomes 的隐形眼镜中的药物浓度更高。隐形眼镜的最佳透光率为 98.02 ± 0.36,膨胀率为 50.35 ± 0.57。浸泡时间延长至 7 天后,隐形眼镜中的药物浓度有所增加。然而,由于隐形眼镜的饱和,在第 7 天后就没有观察到进一步的增加。含溴莫尼定iosomes 的隐形眼镜降低眼内压的效果与市售制剂相似。结论 含有溴莫尼定iosomes 的隐形眼镜通过浸泡法显示出卓越的药物负荷能力,具有最佳的透射比和膨胀系数。浸泡 7 天可增加隐形眼镜中的药物浓度,且不会因饱和而进一步增加。这些镜片与市场上销售的制剂一样能降低眼内压,并能延长释放时间 20 小时。
本文章由计算机程序翻译,如有差异,请以英文原文为准。

Development of brimonidine niosomes laden contact lenses for extended release and promising delivery system in glaucoma treatment

Development of brimonidine niosomes laden contact lenses for extended release and promising delivery system in glaucoma treatment

Background

Increased intraocular pressure is a common symptom of glaucoma. In severe circumstances, it may result in loss of eyesight. Glaucoma treatment is difficult due to ocular physiological barriers that prevent medications from reaching the afflicted area. Traditional formulations (eye drops) have a short residence period and are rapidly drained away via the nasolacrimal duct, resulting in increased adverse drug responses and lower efficacy. The usage of nanoparticles such as niosomes could be one potential answer to these problems. While niosomes improve drug penetration, they have little effect on ocular retention of the medication. Contact lenses containing niosomes can assist to overcome this disadvantage.

Objective

This study aims to prepare and evaluate Brimonidine niosomes laden contact lenses for the treatment of Glaucoma.

Methods

Brimonidine niosomes were prepared using thin film hydration method and evaluated. The contact lenses were soaked in the niosomal formulation at varying intervals (3–10 days). Thereafter, the contact lenses were evaluated for %transmittance, %swelling index, drug quantification and in vitro drug release. The pharmacodynamic studies were conducted to assess the reduction in intraocular pressure (IOP) in albino rabbits. The research compared the results of the reduction in intraocular pressure caused by Brimonidine niosomes laden contact lenses with a marketed preparation of niosomes.

Results

Higher concentration of the drug was loaded in contact lenses loaded with Brimonidine niosomes compared to the marketed formulation, by soaking method. The contact lenses exhibited an optimal %transmittance of 98.02 ± 0.36 and %swelling index of 50.35 ± 0.57. Increase in the soaking time up to 7 days led to an increase in the drug concentration in the contact lenses. However, no further increase was observed after the 7th day due to saturation of the contact lenses. Brimonidine niosomes laden contact lenses provided a reduction in intraocular pressure that was similar to the marketed preparation. Further, the contact lenses provided extended release up to 20 h.

Conclusion

Brimonidine niosomes laden contact lenses exhibited superior drug loading through the soaking method, displaying optimal %transmittance and %swelling index. Soaking for 7 days increased drug concentration in contact lenses with no further increase due to saturation. These lenses reduced intraocular pressure like the marketed formulation, offering extended release for 20 h.

Graphical abstract

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来源期刊
DARU Journal of Pharmaceutical Sciences
DARU Journal of Pharmaceutical Sciences PHARMACOLOGY & PHARMACY-
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期刊介绍: DARU Journal of Pharmaceutical Sciences is a peer-reviewed journal published on behalf of Tehran University of Medical Sciences. The journal encompasses all fields of the pharmaceutical sciences and presents timely research on all areas of drug conception, design, manufacture, classification and assessment. The term DARU is derived from the Persian name meaning drug or medicine. This journal is a unique platform to improve the knowledge of researchers and scientists by publishing novel articles including basic and clinical investigations from members of the global scientific community in the forms of original articles, systematic or narrative reviews, meta-analyses, letters, and short communications.
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