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经皮调制离子电渗和微针递药盐酸罗匹尼罗。

Controlled delivery of ropinirole hydrochloride through skin using modulated iontophoresis and microneedles.

机构信息

College of Pharmacy and Health Sciences, Mercer University, Atlanta, GA 30341, USA.

出版信息

J Drug Target. 2013 May;21(4):354-66. doi: 10.3109/1061186X.2012.757768. Epub 2013 Jan 11.

DOI:10.3109/1061186X.2012.757768
PMID:23311703
Abstract

The objective of this study was to investigate the effect of modulated current application using iontophoresis- and microneedle-mediated delivery on transdermal permeation of ropinirole hydrochloride. AdminPatch® microneedles and microchannels formed by them were characterized by scanning electron microscopy, dye staining and confocal microscopy. In vitro permeation studies were carried out using Franz diffusion cells, and skin extraction was used to quantify drug in underlying skin. Effect of microneedle pore density and ions in donor formulation was studied. Active enhancement techniques, continuous iontophoresis (74.13 ± 2.20 µg/cm(2)) and microneedles (66.97 ± 10.39 µg/cm(2)), significantly increased the permeation of drug with respect to passive delivery (8.25 ± 2.41 µg/cm(2)). Modulated iontophoresis could control the amount of drug delivered at a given time point with the highest flux being 5.12 ± 1.70 µg/cm(2)/h (5-7 h) and 5.99 ± 0.81 µg/cm(2)/h (20-22 h). Combination of modulated iontophoresis and microneedles (46.50 ± 6.46 µg/cm(2)) showed significantly higher delivery of ropinirole hydrochloride compared to modulated iontophoresis alone (84.91 ± 9.21 µg/cm(2)). Modulated iontophoresis can help in maintaining precise control over ropinirole hydrochloride delivery for dose titration in Parkinson's disease therapy and deliver therapeutic amounts over a suitable patch area and time.

摘要

本研究旨在探讨经离子导入和微针介导传递调制电流对盐酸罗匹尼罗经皮渗透的影响。使用扫描电子显微镜、染料染色和共聚焦显微镜对 AdminPatch®微针及其形成的微通道进行了表征。通过 Franz 扩散池进行了体外渗透研究,并采用皮肤提取法定量测定底层皮肤中的药物。研究了微针孔密度和供体配方中离子的影响。主动增强技术,连续离子电渗(74.13 ± 2.20 µg/cm²)和微针(66.97 ± 10.39 µg/cm²),与被动给药(8.25 ± 2.41 µg/cm²)相比,显著增加了药物的渗透。调制离子电渗可以控制在给定时间点输送的药物量,最高通量为 5.12 ± 1.70 µg/cm²/h(5-7 h)和 5.99 ± 0.81 µg/cm²/h(20-22 h)。调制离子电渗和微针的组合(46.50 ± 6.46 µg/cm²)与单独调制离子电渗(84.91 ± 9.21 µg/cm²)相比,盐酸罗匹尼罗的输送量显著增加。调制离子电渗有助于对盐酸罗匹尼罗的输送进行精确控制,以进行帕金森病治疗中的剂量滴定,并在合适的贴片面积和时间内输送治疗量。

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