Department of Pharmacy, Faculty of Medicine, University of Novi Sad, Hajduk Veljkova 3, 21000 Novi Sad, Serbia.
Department of Pharmacy, Faculty of Medicine, University of Novi Sad, Hajduk Veljkova 3, 21000 Novi Sad, Serbia.
Int J Pharm. 2024 Nov 15;665:124675. doi: 10.1016/j.ijpharm.2024.124675. Epub 2024 Sep 17.
Drug molecules can interact with surfactant molecules either in their monomeric form, where the Benesi-Hildebrand equation determines the binding constant, or when a micellar pseudophase is formed, where the Kawamura equation assesses the partition coefficient. Benesi-Hildebrand plots represent the differential absorbance as a function of surfactant concentration below the critical micelle concentration (CMC), while Kawamura plots show this relationship above the CMC, where the drug can influence the CMC and needs consideration. This review aims to provide an overview of methods for evaluating drug-surfactant interactions in aqueous solutions, particularly below and above the CMC, using spectroscopic data. Understanding these interactions is crucial for pharmacodynamics, affecting drug binding, enzymatic activity, and formulation. Various surfactants were analyzed with diphenhydramine hydrochloride, levofloxacin, phenothiazine, moxifloxacin, and chlorpromazine hydrochloride to determine monomeric binding constants, while sulfathiazole, sodium valproate, cefotaxime, losartan, and metformin hydrochloride were assessed for partitioning coefficient values. Errors in Benesi-Hildebrand plots may arise from considering surfactant concentrations above the CMC, while mistakes in Kawamura plots may stem from neglecting to determine the CMC in the presence of drug molecules, which can alter the surfactant's behavior.
药物分子可以与表面活性剂分子以单体形式相互作用,其中 Benesi-Hildebrand 方程确定结合常数,或者形成胶束拟相时,Kawamura 方程评估分配系数。Benesi-Hildebrand 图表示在临界胶束浓度 (CMC) 以下的表面活性剂浓度下微分吸光度作为表面活性剂浓度的函数,而 Kawamura 图则显示 CMC 以上的关系,此时药物会影响 CMC,需要考虑。本综述旨在提供使用光谱数据评估水溶液中药物-表面活性剂相互作用的方法概述,特别是在 CMC 以下和以上。了解这些相互作用对于药效学至关重要,影响药物结合、酶活性和制剂。用盐酸苯海拉明、左氧氟沙星、吩噻嗪、莫西沙星和盐酸氯丙嗪分析了各种表面活性剂,以确定单体结合常数,而磺胺嘧啶、丙戊酸钠、头孢噻肟、洛沙坦和盐酸二甲双胍则评估了分配系数值。Benesi-Hildebrand 图中的误差可能源于考虑 CMC 以上的表面活性剂浓度,而 Kawamura 图中的错误可能源于忽略在药物分子存在下确定 CMC,这会改变表面活性剂的行为。