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磁泳法增强经皮药物传递:机制研究与贴剂设计。

Magnetophoresis for enhancing transdermal drug delivery: Mechanistic studies and patch design.

机构信息

Department of Pharmaceutics, The University of Mississippi, University, MS 38677, USA.

出版信息

J Control Release. 2010 Dec 1;148(2):197-203. doi: 10.1016/j.jconrel.2010.08.015. Epub 2010 Aug 20.

Abstract

Magnetophoresis is a method of enhancement of drug permeation across the biological barriers by application of magnetic field. The present study investigated the mechanistic aspects of magnetophoretic transdermal drug delivery and also assessed the feasibility of designing a magnetophoretic transdermal patch system for the delivery of lidocaine. In vitro drug permeation studies were carried out across the porcine epidermis at different magnetic field strengths. The magnetophoretic drug permeation "flux enhancement factor" was found to increase with the applied magnetic field strength. The mechanistic studies revealed that the magnetic field applied in this study did not modulate permeability of the stratum corneum barrier. The predominant mechanism responsible for magnetically mediated drug permeation enhancement was found to be "magnetokinesis". The octanol/water partition coefficient of drugs was also found to increase when exposed to the magnetic field. A reservoir type transdermal patch system with a magnetic backing was designed for in vivo studies. The dermal bioavailability (AUC(0-6h)) from the magnetophoretic patch system in vivo, in rats was significantly higher than the similarly designed non-magnetic control patch.

摘要

磁泳是一种通过施加磁场来增强药物穿透生物屏障的方法。本研究调查了磁泳经皮药物传递的机制方面,并评估了设计用于传递利多卡因的磁泳经皮贴剂系统的可行性。在不同磁场强度下,通过猪皮进行了体外药物渗透研究。发现磁泳药物渗透“通量增强因子”随施加的磁场强度而增加。机制研究表明,本研究中应用的磁场不会调节角质层屏障的通透性。发现负责磁介导药物渗透增强的主要机制是“磁动”。当药物暴露于磁场时,其辛醇/水分配系数也会增加。设计了一种带有磁性背衬的储库型经皮贴剂系统用于体内研究。在体内,大鼠的磁泳贴剂系统的皮肤生物利用度(AUC(0-6h))明显高于类似设计的非磁性对照贴剂。

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