Pashirova Tatiana N, Lukashenko Svetlana S, Zakharov Sergey V, Voloshina Alexandra D, Zhiltsova Elena P, Zobov Vladimir V, Souto Eliana B, Zakharova Lucia Ya
A.E Arbuzov Institute of Organic and Physical Chemistry, Kazan Scientific Center, Russian Academy of Sciences, 8, ul. Arbuzov, 420088 Kazan, Russian Federation.
Kazan State Technological University, ul. Karla Marksa 68, Kazan, 420015, Russian Federation.
Colloids Surf B Biointerfaces. 2015 Mar 1;127:266-73. doi: 10.1016/j.colsurfb.2015.01.044. Epub 2015 Feb 3.
Aggregation properties of mono (mono-CS) and dicationic (di-CS) surfactants, namely quaternised derivatives of 1,4-diazabicyclo[2.2.2]octane (DABCO), have been evaluated in water and in nutrient broths of different pH, i.e. in Hottinger broth (рН=7.2) and Sabouraud dextrose broth (рН=5.6). Aggregation capacity of surfactants was shown to be responsible for the solubilization properties of a complex composed of a hydrophobic probe (Sudan I) and a selected drug (quercetin), contributing to the antimicrobial activity of this surfactant system. The effect of N-methyl-d-glucamine (NmDg) additive on the antimicrobial activity of mono-CS, and its aggregation and solubilization parameters, has also been evaluated. A substantial decrease in critical micelle concentration (CMC) of cationic surfactants in nutrient broths (up to 60 times) has been reported. Twofold dilution of monocationic surfactant by NmDg slightly changed the CMC of surfactant; however, it provided a remarkable increase in solubilization capacity (∼by 4 times) and decrease in its toxicity. The data anticipate the potential use of DABCO quaternized derivatives as innovative non-toxic delivery systems for hydrophobic drugs.
已评估了单阳离子(单-CS)和双阳离子(双-CS)表面活性剂,即1,4-二氮杂双环[2.2.2]辛烷(DABCO)的季铵化衍生物,在水以及不同pH值的营养肉汤中的聚集特性,即在霍廷格肉汤(pH = 7.2)和沙氏葡萄糖肉汤(pH = 5.6)中的聚集特性。结果表明,表面活性剂的聚集能力决定了由疏水探针(苏丹I)和选定药物(槲皮素)组成的复合物的增溶特性,这有助于该表面活性剂体系的抗菌活性。还评估了N-甲基-D-葡糖胺(NmDg)添加剂对单-CS抗菌活性及其聚集和增溶参数的影响。据报道,营养肉汤中阳离子表面活性剂的临界胶束浓度(CMC)大幅降低(高达60倍)。NmDg将单阳离子表面活性剂稀释两倍,对表面活性剂的CMC影响不大;然而,它显著提高了增溶能力(约4倍)并降低了其毒性。这些数据预示了DABCO季铵化衍生物作为疏水性药物创新无毒递送系统的潜在用途。