Fitzpatrick Dara, Corish John
Department of Chemistry, University College Cork, Ireland.
Int J Pharm. 2006 Nov 15;325(1-2):90-8. doi: 10.1016/j.ijpharm.2006.06.048. Epub 2006 Jul 8.
This paper investigates the release and transport of a range of anionic drugs from liquid crystalline gels using chemical and physical enhancement techniques. Previous papers [Fitzpatrick, D., Corish, J., 2005. Release characteristics of anionic drug compounds from liquid crystalline gels. I. Passive release across non-rate limiting membranes. Int. J. Pharm. 301, 226-236; Fitzpatrick, D., Corish, J., 2006. Release characteristics of anionic drug compounds from liquid crystalline gels. II. The effects of ion pairing and buffering on the passive delivery of anionic drugs across non rate-limiting membranes. Int. J. Pharm.] have reported on the passive release profiles and those resulting from the incorporation of a chemical enhancer in the vehicle. This paper investigates the behaviour of the system under iontophoretic conditions and also under those of combined physical and chemical enhancement. The data presented here are directly comparable to previous work by Nolan et al. [; Nolan, L.M.A., Corish, J., Corrigan, O.I., Fitzpatrick, D., 2006. Combined effects of iontophoretic and chemical enhancement on drug delivery. II. Transport across human and hairless murine skin. Int. J. Pharm., submitted for publication] which investigated the behaviour of cationic compounds under analogous conditions. The iontophoretic release of diclofenac in the presence of model enhancers is thoroughly investigated. It is also shown that a range of anionic drug molecules undergo an electrochemical change during the course of the experiments which leads to their poor detection. This may be a factor in the under reporting of iontophoretic delivery of anionic drugs in the literature. However, it has been shown that the transport of the drugs is greatly enhanced by the application of an iontophoretic current. Results of combined enhancement studies provide a positive basis on which to proceed with in vitro studies of the system across human skin.
本文利用化学和物理增强技术，研究了一系列阴离子药物从液晶凝胶中的释放和传输。此前的论文[菲茨帕特里克，D.，科里什，J.，2005年。阴离子药物化合物从液晶凝胶中的释放特性。I. 跨非限速膜的被动释放。《国际药学杂志》301卷，226 - 236页；菲茨帕特里克，D.，科里什，J.，2006年。阴离子药物化合物从液晶凝胶中的释放特性。II. 离子对和缓冲对阴离子药物跨非限速膜被动递送的影响。《国际药学杂志》]报道了被动释放曲线以及在载体中加入化学增强剂后的释放曲线。本文研究了该系统在离子导入条件下以及物理和化学联合增强条件下的行为。此处给出的数据可直接与诺兰等人之前的工作[；诺兰，L.M.A.，科里什，J.，科里根，O.I.，菲茨帕特里克，D.，2006年。离子导入和化学增强对药物递送的联合作用。II. 跨人和无毛小鼠皮肤的传输。《国际药学杂志》，已提交发表]进行比较，该工作研究了阳离子化合物在类似条件下的行为。深入研究了在模型增强剂存在下双氯芬酸的离子导入释放。研究还表明，一系列阴离子药物分子在实验过程中会发生电化学变化，导致其检测效果不佳。这可能是文献中阴离子药物离子导入递送报道不足的一个因素。然而，研究表明施加离子导入电流可极大地增强药物的传输。联合增强研究的结果为开展该系统跨人皮肤的体外研究提供了积极的基础。
