Department of Chemistry, UGC-Centre for Advanced Studies, Guru Nanak Dev University, Amritsar 143 005, India.
J Colloid Interface Sci. 2012 Dec 1;387(1):194-204. doi: 10.1016/j.jcis.2012.07.085. Epub 2012 Aug 3.
An evaluation of the interactions of phenothiazine tranquilizer drugs (promazine hydrochloride; PMZ and promethazine hydrochloride; PMT) with bile salts viz., sodium cholate (NaC) and sodium deoxycholate (NaDC) in aqueous medium, investigated through different physicochemical measurements is presented in this work. The mixed micellization behavior and surface properties of the phenothiazine-bile salt systems have been analyzed by conductivity and surface tension measurements. Application of different theoretical approaches to all the phenothiazine-bile salt mixtures shows a non-ideal behavior. Further, the spectroscopic techniques such as UV-visible and steady state fluorescence have been employed to study the binding of phenothiazines with bile salts. The stoichiometric ratios, binding constants (K), and free energy change (ΔG) for the phenothiazine-bile salt complexes were estimated from the Benesi-Hildebrand (B-H) double reciprocal plots obtained by using the changes in spectral intensities of phenothiazines on addition of bile salts. The results are discussed in the light of use of bile salts as promising drug delivery agents for phenothiazines and hence improve their bioavailabilty.
本工作通过不同的物理化学测量方法评价了吩噻嗪类镇静剂药物(盐酸普马嗪;PMZ 和盐酸异丙嗪;PMT)与胆汁盐(即胆酸钠(NaC)和脱氧胆酸钠(NaDC))在水介质中的相互作用。通过电导率和表面张力测量分析了吩噻嗪-胆汁盐体系的混合胶束化行为和表面性质。应用不同的理论方法对所有吩噻嗪-胆汁盐混合物的研究表明,其行为是非理想的。此外,还采用了紫外-可见光谱和稳态荧光光谱技术研究了吩噻嗪与胆汁盐的结合。从使用胆汁盐引起的吩噻嗪光谱强度变化获得的 Benesi-Hildebrand(B-H)双倒数图中,估算了吩噻嗪-胆汁盐配合物的化学计量比、结合常数(K)和自由能变化(ΔG)。结果根据胆汁盐作为吩噻嗪类有前途的药物传递剂的用途进行了讨论,从而提高了它们的生物利用度。