Balmanno Alexandra, Falconer James R, Ravuri Halley G, Mills Paul C
School of Veterinary Science, The University of Queensland, Gatton Campus, Gatton, QLD 4343, Australia.
School of Pharmacy, The University of Queensland, Dutton Park Campus, Woolloongabba, QLD 4102, Australia.
Pharmaceutics. 2024 May 16;16(5):675. doi: 10.3390/pharmaceutics16050675.
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.
非甾体抗炎药（NSAIDs）的透皮给药有可能克服与口服NSAIDs使用相关的一些主要缺点，如胃肠道不良事件和顺应性问题。然而，许多新型NSAIDs的溶解度较差，这给将药物制成适合应用于皮肤的制剂带来了挑战，并且可能会限制透皮渗透，特别是如果目标是达到治疗性的全身药物浓度。本综述概述了用于增加难溶性NSAIDs的溶解度并增强其透过皮肤渗透的各种策略，例如载体的改性、皮肤屏障功能的改性或绕过以及使用先进的纳米级制剂。此外，已发现简单但用途广泛的微乳系统是一种经济高效且非常成功的递送难水溶性NSAIDs的技术。
