使用水凝胶给药探针将庆大霉素通过离子电渗疗法输送到兔角膜中。

Iontophoresis-gentamicin delivery into the rabbit cornea, using a hydrogel delivery probe.

作者信息

Frucht-Pery Joseph, Mechoulam Hadas, Siganos Charalambos S, Ever-Hadani Pnina, Shapiro Mervyn, Domb Abraham

机构信息

Department of Ophthalmology, Hadassah University Hospital, P.O. Box 12000, Jerusalem 91120, Israel.

出版信息

Exp Eye Res. 2004 Mar;78(3):745-9. doi: 10.1016/s0014-4835(03)00215-x.

DOI:10.1016/s0014-4835(03)00215-x

PMID:15106954

Abstract

PURPOSE

To evaluate the efficacy of penetration of gentamicin into the cornea of rabbits using iontophoresis with a hydrogel-gentamicin containing probe.

METHODS

Eight of 10 groups (groups 3-10) of 6 rabbits (one eye per rabbit), underwent corneal iontophoresis using soft stable hydroxyethyl methacrylate hydrogel discs (80% water content) loaded with gentamicin sulphate which were mounted on an iontophoresis probe. The studied current intensities were 0, 0.1, 0.3 and 0.6 mAmp, and the durations of iontophoresis were 10 and 60 sec. Two control groups received 1.4% topical drops of gentamicin every 5 min for 1 hr (group 1) or sub-conjunctival injection of 10 mg gentamicin (group 2). Following sacrifice, aqueous humour was taken, corneas were excised, and gentamicin concentration was determined in aqueous humour and cornea samples.

RESULTS

Post-iontophoresis, the concentration of gentamicin in the corneas ranged from high (88.60 +/- 38.64 microg ml(-1)) to very low (0.10 +/- 0.89 microg ml(-1)). Both the control groups and those rabbits treated with current intensity of 0.1 mAmp or greater obtained therapeutic gentamicin levels in the corneas. Use of iontophoresis for 60 sec or current intensity greater than 0.1 mAmp obtained corneal gentamicin levels not different from sub-conjunctival injection. Application of current intensity of 0.1 mAmp or greater gave corneal gentamicin concentrations comparable to topical application of the drug, except when 0.6 mAmp were used for 60 sec (p = 0.05). Increasing current intensity or duration of iontophoresis significantly increased (p = 0.001 for both) gentamicin penetration into the cornea. Current intensity had more influence (Beta2 = 0.40) than duration (Beta2 = 0.13) on drug penetration. A significant interaction was found between the duration of iontophoresis and the current intensity. Very small or no concentrations of the drug were discovered in the anterior chambers of rabbits.

CONCLUSIONS

Iontophoresis using hydrogel-gentamicin probe may deliver therapeutic concentrations of gentamicin into the cornea.

摘要

目的

使用含庆大霉素的水凝胶探针进行离子电渗疗法，评估庆大霉素渗透入兔角膜的疗效。

方法

10组兔子（每组6只，每只兔子一只眼）中的8组（第3 - 10组），使用装载硫酸庆大霉素的柔软稳定的甲基丙烯酸羟乙酯水凝胶圆盘（含水量80%）进行角膜离子电渗疗法，该圆盘安装在离子电渗疗法探针上。研究的电流强度为0、0.1、0.3和0.6毫安，离子电渗疗法的持续时间为10秒和60秒。两个对照组，一组（第1组）每5分钟局部滴注1.4%的庆大霉素，共1小时；另一组（第2组）结膜下注射10毫克庆大霉素。处死后，采集房水，切除角膜，测定房水和角膜样本中的庆大霉素浓度。

结果

离子电渗疗法后，角膜中庆大霉素的浓度范围从高（88.60±38.64微克/毫升）到非常低（0.10±0.89微克/毫升）。对照组以及那些接受0.1毫安或更高电流强度治疗的兔子，角膜中获得了治疗性庆大霉素水平。使用60秒的离子电渗疗法或电流强度大于0.1毫安时，角膜中的庆大霉素水平与结膜下注射无异。施加0.1毫安或更高的电流强度，角膜中的庆大霉素浓度与局部应用该药物相当，但使用0.6毫安持续60秒时除外（p = 0.05）。增加电流强度或离子电渗疗法的持续时间，显著增加了（两者p均 = 0.001）庆大霉素向角膜的渗透。电流强度对药物渗透的影响（β2 = 0.40）大于持续时间（β2 = 0.13）。发现离子电渗疗法的持续时间和电流强度之间存在显著交互作用。在兔子的前房中发现的药物浓度非常低或未发现。