Applied Chemistry Department, Sardar Vallabhbhai National Institute of Technology (SVNIT), Ichchhanath, Surat, 395 007, Gujarat, India.
Department of Chemical Engineering, Sardar Vallabhbhai National Institute of Technology (SVNIT), Ichchhanath, Surat, 395 007, Gujarat, India.
Colloids Surf B Biointerfaces. 2019 Jul 1;179:437-444. doi: 10.1016/j.colsurfb.2019.03.059. Epub 2019 Mar 28.
This work investigates the use of quaternary ammonium based Gemini surfactants (GS) to examine the solubilization and stabilization of a poorly water soluble anti-inflammatory drug Diclofenac (Df). Here we demonstrate the effect of pH on the suspension profile of Df release where it exhibits maximum solubility and absorbance at pH = 10. Interaction process of such cationic GS with Df have been systematically characterized using tensiometry and UV-vis spectroscopy techniques from pre-micellar to post-micellar regions. The spectral results revealed that all the individual GS bind on Df electrostatically resulting in GS + Df complexation. For all the three GS examined, the critical micelle concentration (CMC) was found to decrease in presence of Df following the order: 12-2-12 > 12-2-16 > 16-2-16 which inferred that 12-2-12 can effectively suppress Df degradation at very low concentration. In comparison to 12-2-12, 12-2-16 and 16-2-16 exhibited weaker interaction with Df which limits the stability/solubility of Df in their respective micelles. The aggregation behavior of Df with various GS was investigated by dynamic light scattering (DLS) method. The structural orientation of GS and Df was elucidated by molecular simulation study using Gauss View 5.0.9. The influence of the 12-2-12 in presence of Df on the cervical cell morphology has been undertaken to understand the cytotoxic effect using MTT assay.
本工作研究了季铵盐双子表面活性剂（GS）的应用，以考察其对难溶性抗炎药物双氯芬酸（Df）的增溶和稳定作用。在这里，我们展示了 pH 值对 Df 释放悬浮液特性的影响，在 pH=10 时，Df 表现出最大的溶解度和吸光度。使用界面张力法和紫外可见光谱技术，从胶束前区到胶束后区，系统地表征了这种阳离子 GS 与 Df 的相互作用过程。光谱结果表明，所有的单个 GS 都与 Df 静电相互作用，导致 GS+Df 络合。对于所研究的三种 GS，在 Df 存在下，临界胶束浓度（CMC）均发现降低，顺序为：12-2-12>12-2-16>16-2-16，这表明 12-2-12 可以在非常低的浓度下有效抑制 Df 的降解。与 12-2-12 相比，12-2-16 和 16-2-16 与 Df 的相互作用较弱，限制了 Df 在各自胶束中的稳定性/溶解度。通过动态光散射（DLS）方法研究了 Df 与各种 GS 的聚集行为。使用高斯视图 5.0.9 通过分子模拟研究阐明了 GS 和 Df 的结构取向。通过 MTT 测定法研究了 12-2-12 在存在 Df 的情况下对宫颈细胞形态的影响，以了解细胞毒性作用。
