Chemistry Department, Faculty of Science, King Abdulaziz University, Jeddah, Saudi Arabia.
PLoS One. 2020 Nov 6;15(11):e0241300. doi: 10.1371/journal.pone.0241300. eCollection 2020.
Herein, the interaction among the antidepressant drug amitriptyline hydrochloride (AMT) and a green gemini surfactant, ethane-1, 2-diyl bis(N,N-dimethyl-N-tetradecylammoniumacetoxy) dichloride (14-E2-14), via numerous techniques such as tensiometry, fluorimetry, FT-IR and UV-visible spectroscopy in three different media (aqueous 0.050 mol·kg-1 NaCl, 0.50 and 1.0 mol·kg-1 urea) were investigated. AMT is used to treat mental illness or mood problems, such as depression. The aggregation of biologically active ingredients can enhance the bioavailability of hydrophobic drugs. A significant interaction between AMT and 14-E2-14 was detected by tensiometric study as the critical micelle concentration (cmc) of AMT+14-E2-14 is reduced upon an increase of mole fraction (α1) of 14-E2-14. The decrease in cmc indicates the nonideality of studied mixtures of different compositions. Although, employed drug AMT is freely soluble in the aqueous and non-aqueous system but is not hydrophobic enough to act as its carrier. Instead, gemini surfactant formed spherical micelles in an aqueous system and their high solubilization capability, as well as their relatively lower cmc value, makes them highly stable in vivo. The cmc values of AMT+14-E-14 mixtures in all cases were further decreased and increased in NaCl and urea solutions respectively as compared with the aqueous system. Numerous micellar, interfacial, and thermodynamic parameters have been measured by applying various theoretical models. The obtained changes in the physicochemical assets of AMT upon adding of 14-E2-14 are likely to enhance the industrial and pharmaceutical applications of gemini surfactants. The negative interaction parameters (βm and βσ), indicate synergistic attraction is occurring in the mixed systems. The aggregation number (Nagg), Stern-Volmer constant (Ksv), etc. are attained through the fluorescence method, also supporting the attractive interaction behavior of AMT+14-E2-14 mixtures in all solvents. The Nagg was found to increase in the salt solution and decrease in the urea system compared with the aqueous solution. FT-IR and UV-visible analysis also depict the interaction between the constituent alike tensiometry and fluorimetry methods. The results suggested that gemini surfactants may serve as a capable drug delivery agent for antidepressants, improving their bioavailability.
本文通过张力计、荧光光谱法、FT-IR 和紫外可见光谱法等多种技术研究了抗抑郁药盐酸阿米替林(AMT)与绿色双子表面活性剂乙烷-1,2-二基双(N,N-二甲基-N-十四烷基铵乙氧基)二氯化物(14-E2-14)在三种不同介质(0.050 mol·kg-1 NaCl 水溶液、0.50 和 1.0 mol·kg-1 尿素)中的相互作用。AMT 用于治疗精神疾病或情绪问题,如抑郁症。生物活性成分的聚集可以提高疏水性药物的生物利用度。张力计研究表明,AMT 和 14-E2-14 之间存在显著相互作用,因为 14-E2-14 的摩尔分数(α1)增加时,AMT+14-E2-14 的临界胶束浓度(cmc)降低。cmc 的降低表明不同组成的研究混合物是非理想的。尽管,所使用的药物 AMT 在水相和非水相系统中均具有高溶解度,但它的疏水性不足以作为其载体。相反,双子表面活性剂在水相中形成球形胶束,其高增溶能力以及相对较低的 cmc 值使它们在体内高度稳定。与水相相比,在所有情况下,AMT+14-E-14 混合物的 cmc 值在 NaCl 和尿素溶液中分别降低和增加。通过应用各种理论模型测量了大量胶束、界面和热力学参数。在添加 14-E2-14 后,AMT 的物理化学性质发生变化,可能会增强双子表面活性剂的工业和制药应用。负相互作用参数(βm 和 βσ)表明混合体系中存在协同吸引力。通过荧光法获得的聚集数(Nagg)、斯特恩-沃尔默常数(Ksv)等,也支持 AMT+14-E2-14 混合物在所有溶剂中的吸引力相互作用行为。与水相相比,在盐溶液中,Nagg 增加,而在尿素体系中,Nagg 减少。FT-IR 和紫外可见分析也描绘了张力计和荧光光谱法等组成相似的相互作用。结果表明,双子表面活性剂可以作为抗抑郁药的有效药物输送剂,提高其生物利用度。