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使用水凝胶离子电渗疗法将甲基强的松龙递送至眼后部。

Methylprednisolone delivery to the back of the eye using hydrogel iontophoresis.

作者信息

Eljarrat-Binstock Esther, Orucov Faik, Frucht-Pery Joseph, Pe'er Jacob, Domb Abraham J

机构信息

Department of Medicinal Chemistry and Natural Products, School of Pharmacy, Faculty of Medicine, The Hebrew University of Jerusalem, Jerusalem, Israel.

出版信息

J Ocul Pharmacol Ther. 2008 Jun;24(3):344-50. doi: 10.1089/jop.2007.0097.

Abstract

AIM

The aim of this study was to evaluate methylprednisolone penetration into ocular structures after low-current trans-scleral hydrogel iontophoresis, as compared with the common intravenous (i.v.) treatment.

METHODS

Methylprednisolone hemisuccinate (MPH) iontophoresis was studied in rabbits, using drug-loaded hydrogels mounted on a portable iontophoretic device. Cathodal iontophoresis of 2.6 mA/cm(2) was applied for 5 min at two opposite sites on the sclera or for 10 min at the same site. Ocular drug levels were determined 2 h after iontophoretic treatment, then compared to mock iontophoresis and i.v. infusion of 10 mg/kg methylprednisolone.

RESULTS

Significantly higher methylprednisolone levels were found in ocular tissues after iontophoresis, compared with the control groups, except for the sclera concentrations, which were similar to the concentrations achieved after mock iontophoresis. Two (2) h after the trans-scleral iontophoretic treatment, 178.59 +/- 21.63 microg/g, 6.74 +/- 2.38 microg/ml, and 2.71 +/- 0.57 microg/mL were found in the retina, aqueous humor, and vitreous, respectively. No significant differences were found between one or two site treatments of trans-scleral iontophoresis. Nondetectable concentrations were found 2 h after the i.v. infusion of 10 mg/kg of methylprednisolone in all evaluated ocular tissues and fluids.

CONCLUSIONS

A short, low-current noninvasive iontophoretic treatment, using methylprednisolone-loaded hydrogels, has potential clinical value in treating ocular inflammatory diseases.

摘要

目的

本研究旨在评估与普通静脉注射治疗相比,低电流经巩膜水凝胶离子电渗疗法后甲泼尼龙在眼内结构中的渗透情况。

方法

在兔身上研究甲泼尼龙半琥珀酸酯(MPH)离子电渗疗法,使用安装在便携式离子电渗装置上的载药水凝胶。在巩膜的两个相对部位施加2.6 mA/cm²的阴极离子电渗疗法5分钟,或在同一部位施加10分钟。离子电渗治疗后2小时测定眼内药物水平,然后与假离子电渗疗法和静脉注射10 mg/kg甲泼尼龙进行比较。

结果

与对照组相比,离子电渗疗法后眼组织中的甲泼尼龙水平显著更高,但巩膜浓度除外,其与假离子电渗疗法后达到的浓度相似。经巩膜离子电渗治疗后2小时,视网膜、房水和玻璃体中的浓度分别为178.59±21.63μg/g、6.74±2.38μg/ml和2.71±0.57μg/mL。经巩膜离子电渗疗法的一个或两个部位治疗之间未发现显著差异。静脉注射10 mg/kg甲泼尼龙2小时后,在所有评估的眼组织和液体中均未检测到浓度。

结论

使用载有甲泼尼龙的水凝胶进行短时间、低电流的非侵入性离子电渗治疗在治疗眼部炎症性疾病方面具有潜在的临床价值。

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