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Interaction of Surface Active Drug Promethazine Hydrochloride with Surfactants: Drug Release from Microemulsions
Tenside Surfactants Detergents ( IF 1 ) Pub Date : 2021-09-25 , DOI: 10.1515/tsd-2020-2351
Manoni Kurtanidze 1 , Tinatin Butkhuzi 1 , Irma Tikanadze 1 , Rusudan Chaladze 1 , Manuchar Gvaramia 2 , Ketevan Nanobashvili 1 , Maka Alexishvili 3 , Polina Toidze 4 , Marina Rukhadze 1
Affiliation  

The interaction of surface-active drugs with surfactants, used in the simulation of artificial membranes by direct and reversed micelles, mainly determines the transport of drugs in the body and the complex process of the binding to receptors. Besides, the delivery of drugs into the body via microemulsions has been successfully used to reduce the first-pass metabolism. The structure of mixed reverse microemulsions based on the ionic surfactant sodium bis(2-ethylhexyl)sulfosuccinate (AOT) and the cationic surface active drug promethazine hydrochloride (PMT) was studied spectroscopically in the infrared and UV-visible regions, as well as using electrical conductivity and dynamic light scattering. The release profile of PMT from AOT-based microemulsions was studied using cellulose dialysis bags. The introduction of PMT additive into the water pockets of reverse AOT micelles leads to: a) an increase in free water fraction and a decrease in bound water fraction; b) changing the chromatographic retention factors of the model compounds; c) insignificant influence on the values of the binding constant of optical probe o-nitroaniline with the head groups of AOT; d) quenching of water-induced percolation in electrical conductance of reverse AOT microemulsions; e) a slight decrease in the size of water droplets at the same values of the molar ratio of water/surfactant. The release of PMT from the aqueous system obeys Fick’s law of diffusion (n = 0.4852), and the release of PMT from microemulsions is based on non-Fickian or anomalous diffusion.

中文翻译:

表面活性药物盐酸异丙嗪与表面活性剂的相互作用:药物从微乳中释放

表面活性药物与表面活性剂的相互作用,用于通过直接胶束和反胶束模拟人工膜,主要决定药物在体内的转运和与受体结合的复杂过程。此外,通过微乳将药物输送到体内已成功地用于减少首过代谢。以离子表面活性剂双(2-乙基己基)磺基琥珀酸钠(AOT)和阳离子表面活性药物盐酸异丙嗪(PMT)为基础的混合反相微乳液的结构在红外和紫外可见光谱以及电电导率和动态光散射。使用纤维素透析袋研究了基于 AOT 的微乳液中 PMT 的释放曲线。将 PMT 添加剂引入反相 AOT 胶束的水囊会导致: a) 游离水部分增加,结合水部分减少;b) 改变模型化合物的色谱保留因子;c) 对光学探针结合常数值的影响不显着-具有AOT头基的硝基苯胺;d) 淬灭反向 AOT 微乳液的电导中的水诱导渗透;e) 在水/表面活性剂的摩尔比相同的情况下,水滴尺寸略有减小。PMT 从水系统中的释放遵循 Fick 扩散定律 (n = 0.4852),而 PMT 从微乳液中的释放是基于非 Fickian 或反常扩散。
更新日期:2021-09-25
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