Application of confocal laser scanning microscopy in characterization of chemical enhancers in drug-in-adhesive transdermal patches

AAPS PharmSci Pub Date : 2002-03-01 DOI:10.1208/ps040103
M. H. Qvist, U. Hoeck, B. Kreilgaard, F. Madsen, L. Hovgaard, S. Frokjaer
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引用次数: 11

Abstract

The purpose of this study was to evaluate the application of confocal laser scanning microscopy (CLSM) in the examination of the embedment and the release characteristics of chemical permeation enhancers from transdermal drug delivery systems (TDDSs) of the “drug-in-adhesive” type. The enhancer lauric acid and a lauric acid fluorescing probe of the Bodipy type were incorporated into TDDSs consisting of an acrylic, a polyisobutylene, or a silicone polymer adhesive. Three-dimensional confocal images of the distribution were obtained before and during release into an aqueous medium. The images showed that the lauric acid fluorescing probe was homogeneously embedded in all the adhesives except for 1 polyisobutylene. The release profiles and release rate constants of the lauric acid fluorescing probe were consistent with data from a release study of lauric acid performed using conventional measurements of the released amounts. This indicated that lauric acid was distributed in a homogeneous manner. Furthermore, it was possible to illustrate the mechanics of the diffusion process inside the TDDS and compare these patterns with theoretically drawn profiles, based on Ficks law of diffusion. CLSM was demonstrated to be an excellent tool to study how enhancers are incorporated and diffuse into a TDDS.
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激光共聚焦扫描显微镜在药物黏附透皮贴剂化学增强剂表征中的应用
本研究的目的是评价共聚焦激光扫描显微镜(CLSM)在“黏附药”型透皮给药系统(TDDSs)中化学渗透促进剂的包埋和释放特性。将增强剂月桂酸和Bodipy型月桂酸荧光探针掺入由丙烯酸、聚异丁烯或有机硅聚合物粘合剂组成的TDDSs中。在释放到水介质之前和释放过程中获得了三维共聚焦图像。结果表明,月桂酸荧光探针除1聚异丁烯外,均均匀嵌入胶粘剂中。月桂酸荧光探针的释放曲线和释放速率常数与使用常规释放量测量进行的月桂酸释放研究的数据一致。这表明月桂酸的分布是均匀的。此外,还可以说明TDDS内部扩散过程的机制,并将这些模式与基于菲克斯扩散定律的理论绘制的轮廓进行比较。CLSM被证明是研究增强剂如何被纳入和扩散到TDDS的一个很好的工具。
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