Milanowski Bartłomiej, Wosicka-Frąckowiak Hanna, Główka Eliza, Sosnowska Małgorzata, Woźny Stanisław, Stachowiak Filip, Suchenek Angelika, Wilkowski Dariusz
Chair and Department of Pharmaceutical Technology, Poznan University of Medical Sciences, ul. Grunwaldzka 6, 60-780 Poznań, Poland.
GENERICA Pharmaceutical Lab, Regionalne Centrum Zdrowia Sp. z o. o., ul. Na Kępie 3, 64-360 Zbąszyń, Poland.
Pharmaceutics. 2021 Aug 20;13(8):1305. doi: 10.3390/pharmaceutics13081305.
Pharmaceutical products containing non-steroidal anti-inflammatory drugs (NSAIDs) are among the most prescribed topical formulations used for analgesic and antirheumatic properties. These drugs must overcome the skin barrier to cause a therapeutic effect. Human skin has been widely used as a model to study in vitro drug diffusion and permeation, however, it suffers from many limitations. Therefore, to perform in vitro permeation test (IVPT), we used a Strat-M membrane with diffusion characteristics well-correlated to human skin. This study's objective was to optimize the IVPT conditions using Plackett-Burman experimental design for bio-predictive evaluation of the in vitro permeation rates of five non-steroidal anti-inflammatory drugs (diclofenac, etofenamate, ibuprofen, ketoprofen, naproxen) across Strat-M membrane from commercial topical formulations. The Plackett-Burman factorial design was used to screen the effect of seven factors in eight runs with one additional center point. This tool allowed us to set the sensitive and discriminative IVPT final conditions that can appropriately characterize the NSAIDs formulations. The permeation rate of etofenamate (ETF) across the Strat-M membrane was 1.7-14.8 times faster than other NSAIDs from selected semisolids but 1.6 times slower than the ETF spray formulation.
含有非甾体抗炎药（NSAIDs）的药品是用于止痛和抗风湿特性的最常用外用制剂之一。这些药物必须克服皮肤屏障才能产生治疗效果。人体皮肤已被广泛用作研究体外药物扩散和渗透的模型，然而，它存在许多局限性。因此，为了进行体外渗透试验（IVPT），我们使用了一种Strat-M膜，其扩散特性与人体皮肤高度相关。本研究的目的是使用Plackett-Burman实验设计优化IVPT条件，以便对五种非甾体抗炎药（双氯芬酸、依托芬那酯、布洛芬、酮洛芬、萘普生）从市售外用制剂透过Strat-M膜的体外渗透速率进行生物预测评估。Plackett-Burman析因设计用于在八次运行中筛选七个因素的影响，并增加一个中心点。该工具使我们能够设定敏感且有区分性的IVPT最终条件，从而能够恰当地表征NSAIDs制剂。依托芬那酯（ETF）透过Strat-M膜的渗透速率比所选半固体制剂中的其他NSAIDs快1.7至14.8倍，但比ETF喷雾制剂慢1.6倍。
