Low frequency sonophoresis mediated transdermal and intradermal delivery of ketoprofen
Low frequency sonophoresis mediated transdermal and intradermal delivery of ketoprofen
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DOI：
10.1016/j.ijpharm.2011.11.041
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发表时间：
2012-02-28
影响因子：
5.8
通讯作者：
Banga, Ajay K.
中科院分区：
文献类型：
--
作者：
Herwadkar, Anushree;Sachdeva, Vishal;Banga, Ajay K.
本研究的目的是测试在20 kHz下的低频超声促渗用于将酮洛芬递送到皮肤中和穿过皮肤。使用Franz扩散池在体外对切除的无毛大鼠皮肤进行24小时的渗透研究，之后对皮肤样品进行皮肤提取以定量皮肤中存在的药物量。优化了超声施加时间、占空比耦合介质和超声喇叭距皮肤的距离等参数。测量经表皮水分损失（TEWL）以指示超声波促渗后屏障破坏的程度。使用共聚焦显微镜观察染料渗透通过超声促渗处理的皮肤。应用超声显著增强了酮洛芬的渗透，从被动递送的74.87 +/- 5.27 μ g/cm（2）增加到超声促渗的491.37 +/- 48.78 μ g/cm（2）。皮肤层中的药物水平从被动渗透后的34.69 +/- 7.25 μ g增加到超声促渗后的212.62 +/- 45.69 μ g。TEWL从31.6 +/- 0.02（被动）增加到69.5 +/- 12.60（超声促渗），表明屏障特性被破坏。共聚焦显微镜图像描绘了通过超声促渗处理的皮肤的增强的染料渗透，证实了屏障破坏。优化超声参数的低频超声导入法可有效地促进酮洛芬的透皮和局部给药。(C)2011 Elsevier B. V.保留所有权利。
The objective of this study was to test low frequency sonophoresis at 20 kHz for delivery of ketoprofen into and across the skin. Permeation studies were carried out in vitro on excised hairless rat skin over a period of 24 h using Franz diffusion cells after which, skin samples were subjected to skin extraction to quantify the amount of drug present in skin. Parameters like ultrasound application time, duty cycle coupling medium and distance of ultrasound horn from skin were optimized. Transepidermal water loss (TEWL) was measured to indicate the extent of barrier disruption following sonophoresis. Confocal microscopy was used to visualize dye penetration through sonophoresis treated skin. Application of ultrasound significantly enhanced permeation of ketoprofen from 74.87 +/- 5.27 mu g/cm(2) for passive delivery to 491.37 +/- 48.78 mu g/cm(2) for sonophoresis. Drug levels in skin layers increased from 34.69 +/- 7.25 mu g following passive permeation to 212.62 +/- 45.69 mu g following sonophoresis. TEWL increased from 31.6 +/- 0.02 (passive) to 69.5 +/- 12.60 (sonophoresis) indicating disruption of barrier properties. Confocal microscopy images depicted enhanced dye penetration through sonophoresis treated skin confirming barrier disruption. Low frequency sonophoresis with optimized ultrasound parameters can be effectively used to actively enhance transdermal and topical delivery of ketoprofen. (C) 2011 Elsevier B.V. All rights reserved.