Ossowicz-Rupniewska Paula, Nowak Anna, Konopacki Maciej, Kordas Marian, Kucharski Łukasz, Klebeko Joanna, Świątek Ewelina, Rakoczy Rafał
West Pomeranian University of Technology in Szczecin, Faculty of Chemical Technology and Engineering, Department of Chemical Organic Technology and Polymeric Materials, Piastów Ave. 42, 71-065 Szczecin, Poland.
Pomeranian Medical University in Szczecin, Department of Cosmetic and Pharmaceutical Chemistry, Powstańców Wielkopolskich Ave. 72, 70-111 Szczecin, Poland.
Eur J Pharm Biopharm. 2023 Jul;188:15-25. doi: 10.1016/j.ejpb.2023.05.003. Epub 2023 May 8.
A method of increasing the permeability of ibuprofen through the skin using a rotating magnetic field (RMF) is presented. This study evaluated whether 50 Hz RMF modifies ibuprofen's permeability through the skin. Ibuprofen and its structural modifications in the form of ibuprofenates of isopropyl esters of L-amino acids such as L-valine, L-phenylalanine, L-proline, and L-aspartic acid were used in the research. To this end, Franz cells with skin as membrane were exposed to 50 Hz RMF with 5% ibuprofen and its derivatives in an ethanol solution for 48 h. Following the exposures, the amount of penetrated compound was analysed. Regardless of the compound tested, a significant increase in drug transport through the skin was observed. The differences in the first 30 min of permeation are particularly noticeable. Furthermore, it was shown that using RMF increases the permeability of ibuprofen from 4 to 244 times compared to the test without the RMF. The greatest differences were observed for unmodified ibuprofen. However, it is noteworthy that the largest amounts of the active substance were obtained with selected modifications and exposure to RMF. The RMF may be an innovative and interesting technology that increases the penetration of anti-inflammatory and anti-ache drugs through the skin.
本文提出了一种利用旋转磁场(RMF)提高布洛芬经皮渗透性的方法。本研究评估了50Hz的旋转磁场是否会改变布洛芬的经皮渗透性。研究中使用了布洛芬及其L-氨基酸异丙酯(如L-缬氨酸、L-苯丙氨酸、L-脯氨酸和L-天冬氨酸)的布洛芬酯形式的结构修饰物。为此,将以皮肤为膜的弗兰兹扩散池暴露于含有5%布洛芬及其衍生物的乙醇溶液中的50Hz旋转磁场中48小时。暴露后,分析渗透化合物的量。无论测试的化合物如何,均观察到药物经皮转运显著增加。渗透前30分钟的差异尤为明显。此外,结果表明,与无旋转磁场的测试相比,使用旋转磁场可使布洛芬的渗透性提高4至244倍。未修饰的布洛芬差异最大。然而,值得注意的是,通过选择修饰物并暴露于旋转磁场可获得最大量的活性物质。旋转磁场可能是一种创新且有趣的技术,可提高抗炎和止痛药物的经皮渗透率。