Safety evaluation and pharmacodynamics of minocycline hydrochloride eye drops.

IF 1.8 3区医学 Q4 BIOCHEMISTRY & MOLECULAR BIOLOGY Molecular Vision Pub Date : 2022-01-01

Xiaoli Li, Wenhua Zhang, Zhiqiang Ye, Shuaili Pei, Dongliang Zheng, Lin Zhu

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Abstract

Purpose: This study evaluated the safe dosage of minocycline hydrochloride (Mino) eye drops and investigated the potential for the prevention or reduction of retinal damage in a diabetic rat model.

Methods: Various concentrations of Mino were applied to human corneal epithelial cells (HCECs) to determine the half maximal inhibitory concentration (IC₅₀). The safety of Mino eye drops was evaluated on Sprague-Dawley (SD) rat eyes by slit-lamp examination, electroretinography (ERG), histology, and TUNEL assay. Eye drops (1 mg/ml) were applied to the streptozotocin-induced diabetic SD rats. Clinical observations, ERG analyses, and optical coherence tomography analyses were performed monthly for five months. Eyes were then analyzed via histology, blood-retinal barrier function assay, and retinal vascular staining.

Results: Cytotoxicity analysis using HCECs revealed that the IC₅₀ was 250 µg/ml. Safety analyses in healthy SD rats showed that Mino eye drops did not demonstrate any ocular toxicity. Pharmacodynamics analysis showed that retinal thickness at three months was greater in the Mino group than in the non treated (NT) group. The peak times and amplitudes of each program were better in the Mino group than in the NT group at each time point by ERG analyses. Histology examinations showed a thinner ganglion cell layer, fewer ganglion cells, and more dilated blood vessels in the NT group than in the Mino group.

Conclusion: Mino eye drops at 1 mg/ml were safe when used in SD rats. Mino eye drops can protect the retina from the development or progression of diabetic retinopathy.

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盐酸米诺环素滴眼液的安全性评价及药效学研究。

目的:评价盐酸米诺环素(Mino)滴眼液的安全剂量，探讨其预防或减轻糖尿病大鼠视网膜损伤的可能性。方法:将不同浓度的Mino作用于人角膜上皮细胞(HCECs)，测定其最大半数抑制浓度(IC50)。采用裂隙灯检查、视网膜电图(ERG)、组织学和TUNEL法评价米诺滴眼液在SD大鼠眼上的安全性。采用滴眼液(1 mg/ml)治疗链脲佐菌素诱导的糖尿病SD大鼠。临床观察、ERG分析和光学相干断层扫描分析每月进行5个月。然后通过组织学、血视网膜屏障功能测定和视网膜血管染色对眼睛进行分析。结果:HCECs细胞毒性分析显示IC50为250µg/ml。对健康SD大鼠的安全性分析表明，Mino滴眼液没有任何眼部毒性。药效学分析显示，Mino组3个月时视网膜厚度大于未治疗组(NT)。ERG分析显示，Mino组各节目在各时间点的峰值时间和振幅均优于NT组。组织学检查显示NT组比Mino组神经节细胞层更薄，神经节细胞更少，血管扩张更多。结论:1 mg/ml剂量的米诺滴眼液对SD大鼠是安全的。米诺滴眼液可以保护视网膜免受糖尿病视网膜病变的发展或进展。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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来源期刊

Molecular Vision 生物-生化与分子生物学

CiteScore

4.40

自引率

0.00%

发文量

审稿时长

1 months

期刊介绍： Molecular Vision is a peer-reviewed journal dedicated to the dissemination of research results in molecular biology, cell biology, and the genetics of the visual system (ocular and cortical). Molecular Vision publishes articles presenting original research that has not previously been published and comprehensive articles reviewing the current status of a particular field or topic. Submissions to Molecular Vision are subjected to rigorous peer review. Molecular Vision does NOT publish preprints. For authors, Molecular Vision provides a rapid means of communicating important results. Access to Molecular Vision is free and unrestricted, allowing the widest possible audience for your article. Digital publishing allows you to use color images freely (and without fees). Additionally, you may publish animations, sounds, or other supplementary information that clarifies or supports your article. Each of the authors of an article may also list an electronic mail address (which will be updated upon request) to give interested readers easy access to authors.