改善水溶性差的非甾体抗炎药透皮给药的策略

Alexandra Balmanno, J. Falconer, H. G. Ravuri, Paul C. Mills
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摘要

非甾体抗炎药(NSAIDs)的透皮给药有可能克服口服 NSAIDs 的一些主要缺点,如胃肠道不良反应和依从性。然而,许多新型非甾体抗炎药的溶解度较低,这给将药物纳入适合皮肤应用的制剂带来了挑战,并可能限制透皮渗透,尤其是如果目标是治疗全身性药物浓度的话。本综述概述了用于提高溶解性差的非甾体抗炎药的溶解度并增强其透皮渗透性的各种策略,如改变载体、改变或绕过皮肤屏障功能以及使用先进的纳米级制剂。此外,研究还发现,简单但用途广泛的微乳剂系统是一种成本效益高且非常成功的技术,可用于递送水溶性较差的非甾体抗炎药。
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Strategies to Improve the Transdermal Delivery of Poorly Water-Soluble Non-Steroidal Anti-Inflammatory Drugs
The transdermal delivery of non-steroidal anti-inflammatory drugs (NSAIDs) has the potential to overcome some of the major disadvantages relating to oral NSAID usage, such as gastrointestinal adverse events and compliance. However, the poor solubility of many of the newer NSAIDs creates challenges in incorporating the drugs into formulations suitable for application to skin and may limit transdermal permeation, particularly if the goal is therapeutic systemic drug concentrations. This review is an overview of the various strategies used to increase the solubility of poorly soluble NSAIDs and enhance their permeation through skin, such as the modification of the vehicle, the modification of or bypassing the barrier function of the skin, and using advanced nano-sized formulations. Furthermore, the simple yet highly versatile microemulsion system has been found to be a cost-effective and highly successful technology to deliver poorly water-soluble NSAIDs.
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