Department of Chemistry, Aligarh Muslim University, Aligarh 202002, India.
Department of Chemistry, Aligarh Muslim University, Aligarh 202002, India.
Spectrochim Acta A Mol Biomol Spectrosc. 2019 May 15;215:249-259. doi: 10.1016/j.saa.2019.02.082. Epub 2019 Feb 21.
Knowledge of binding parameters for drug and surfactant complexations is crucially vital in order to design effective drug carrier systems with requisite features. To this end, this work was designed to demonstrate the biophysical characterization of the interaction of a phenothiazine drug promethazine hydrochloride (PMT) with relatively lower cytotoxic and easily degradable biomimetic micellar self-assemblies of oxy-diester functionalized gemini surfactants (C-E2O-C, m = 12, 14 and 16), possessing different hydrophobic character. The binding propensity of C-E2O-C increases upon increasing the hydrophobic tail length as manifested through both intrinsic fluorescence and absorption spectral profiles of PMT ̶ C-E2O-C, showing 1:1 stoichiometry. K values also follow the trend of increasing hydrophobic character (i.e., C-E2O-C < C-E2O-C < C-E2O-C). Moreover, the determined thermodynamic parameters, particularly the positive values of ΔH and ΔS, reveal that the involved complexations are dominated by the hydrophobic interactions. In addition, micropolarity assay was done to deduce the microenvironmental changes upon PMT ̶ C-E2O-C complexations. Beside this, comparative appraisal of all the three systems helps to underpin a reasonable knowledge of the effect of structural variation of surfactants on their binding ability with drug which, in turn, may also open new avenues for the designing of potential tunable drug carrier systems.
为了设计具有必要特性的有效药物载体系统,了解药物和表面活性剂配合物的结合参数至关重要。为此,本工作旨在展示具有较低细胞毒性且易于降解的仿生两亲胶束自组装物氧二酯功能化双子表面活性剂(C-E2O-C,m=12、14 和 16)与吩噻嗪类药物盐酸普罗米嗪(PMT)相互作用的生物物理特性。C-E2O-C 的结合倾向随着疏水性尾链长度的增加而增加,这可以通过 PMT-C-E2O-C 的本征荧光和吸收光谱曲线来证明,表明其具有 1:1 的化学计量比。K 值也遵循疏水性增加的趋势(即,C-E2O-C < C-E2O-C < C-E2O-C)。此外,测定的热力学参数,特别是正值的ΔH 和ΔS,表明所涉及的配合物主要由疏水相互作用主导。此外,还进行了微极性测定,以推断 PMT-C-E2O-C 配合物形成后微环境的变化。除此之外,对所有三个系统的比较评估有助于深入了解表面活性剂结构变化对其与药物结合能力的影响,这反过来也可能为设计潜在的可调药物载体系统开辟新途径。