Mateus Rita, Moore David J, Hadgraft Jonathan, Lane Majella E
Department of Pharmaceutics, UCL School of Pharmacy, 29-39 Brunswick Square, London WC1 N 1AX, United Kingdom.
International Specialty Products, Wayne, NJ, USA; Department of Chemistry, Rutgers University, Newark College of Arts and Sciences, Newark, NJ, USA.
Int J Pharm. 2014 Nov 20;475(1-2):471-4. doi: 10.1016/j.ijpharm.2014.08.061. Epub 2014 Aug 29.
Salicylic acid (SA) has been used in pharmaceutical and cosmetic preparations for many years. Although there are a number of studies which report on the permeation characteristics of this molecule in vitro, to our knowledge the disposition of SA in vivo has not been studied in detail. In the present work we prepared a range of SA formulations with different gelling agents. Permeation of SA from the formulations was studied in vitro using conventional Franz cells and in vivo using confocal Raman spectroscopy (CRS). Selection of the gelling agent clearly influenced the efficacy of SA delivery from all formulations. It was possible to detect SA in vivo using CRS and to depth profile the molecule. A good in vitro-in vivo correlation was also found when the cumulative amounts of SA which permeated in vitro were plotted against the CRS signal in the skin. The findings provide further confidence in the application of CRS for the study of drug disposition in the skin.
水杨酸(SA)已在制药和化妆品制剂中使用多年。尽管有许多研究报告了该分子的体外渗透特性,但据我们所知,SA在体内的处置情况尚未得到详细研究。在本研究中,我们制备了一系列含有不同凝胶剂的SA制剂。使用传统的Franz扩散池体外研究了SA从制剂中的渗透情况,并使用共焦拉曼光谱(CRS)体内研究了SA的渗透情况。凝胶剂的选择明显影响了所有制剂中SA的递送效果。使用CRS可以在体内检测到SA,并对该分子进行深度剖析。当将体外渗透的SA累积量与皮肤中的CRS信号作图时,还发现了良好的体外-体内相关性。这些发现为CRS在皮肤药物处置研究中的应用提供了进一步的信心。