The interaction of a model active pharmaceutical with cationic surfactant and the subsequent design of drug based ionic liquid surfactants

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• 作者：Sara Qamar^a ; ¹ ; Paul Brown^b ; ¹ ; Steven Ferguson^c ; Rafaqat Ali Khan^a ; Bushra Ismail^a ; Abdur Rahman Khan^a ; Murtaza Sayed^a ; Asad Muhammad Khan^a ; ^{amk.qau@gmail.com" class="auth_mail" title="E-mail the corresponding author}
• 关键词：Ionic liquid ; Drug delivery ; UV&ndash ; Vis spectroscopy ; Micelles ; Encapsulation ; Hydrophilic drugs ; Ionic surfactant
• 刊名：Journal of Colloid and Interface Science
• 出版年：2016
• 出版时间：1 November 2016
• 年：2016
• 卷：481
• 期：Complete
• 页码：117-124
• 全文大小：1296 K

文摘

Interactions of active pharmaceutical ingredients (API) with surfactants remain an important research area due to the need to improve drug delivery systems. In this study, UV–Visible spectrophotometry was used to investigate the interactions between a model low molecular weight hydrophilic drug sodium valproate (SV) and cationic surfactant cetyltrimethylammonium bromide (CTAB). Changes in the spectra of SV were observed in pre- and post-micellar concentrations of CTAB. The binding constant (K_b) values and the number of drug molecules encapsulated per micelle were calculated, which posed the possibility of mixed micelle formation and strong complexation between SV and CTAB. These results were compared to those of a novel room temperature surface active ionic liquid, which was synthesized by the removal of inorganic counterions from a 1:1 mixture of CTAB and SV. In this new compound the drug now constitutes a building block of the carrier and, as such, has considerably different surfactant properties to its building blocks. In addition, enhanced solubility in a range of solvents, including simulated gastric fluid, was observed. The study provides valuable experimental evidence concerning the performance of drug based surfactant ionic liquids and how their chemical manipulation, without altering the architecture of the API, leads to control of surfactant behavior and physicochemical properties. In turn, this should feed through to improved and controlled drug release rates and delivery mechanisms, and the prevention of precipitation or formation of polymorphs typical of crystalline form APIs.