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Partitioning of anticancer drug 5-fluorouracil in micellar media explored by physicochemical properties and energetics of interactions: Quantitative insights for implications in drug delivery.
Colloids and Surfaces B: Biointerfaces ( IF 5.8 ) Pub Date : 2019-12-31 , DOI: 10.1016/j.colsurfb.2019.110730
Moumita Dasgupta 1 , Eva Judy 1 , Nand Kishore 1
Affiliation  

Drug delivery vehicles such as micelles, vesicles and other nanoemulsions are necessary for enhanced bioavailability of drugs in the body. We have measured and correlated physicochemical properties of an anticancer drug 5-fluorouracil in the micelles of anionic surfactant sodium dodecyl sulfate. cationic surfactant hexadecyltrimethylammonium bromide, and non-ionic surfactant triton X-100 with the energetics of interactions. Thermodynamic signatures accompanying the partitioning of drug into surfactant micelles along with standard partial molar volume and standard partial molar compressibilities of transfer from water to the micelles have been interpreted in terms of strength, nature and extent of partitioning. Functional groups on the drug responsible for interaction/partitioning in micelles have been identified. Interaction of 5-fluorouracil in two or three sequential partitioning behavior depending on the nature of the surfactant micelles has enabled detailed mechanistic analysis of the partitioning process. Structure-property-energetics relationship to obtain deeper insights into the nature of interaction between the drug and micelles has been addressed. Such studies provide information on the significance of functional groups on the drug molecule which can be modified for optimum partitioning in drug delivery vehicles to account for effective target oriented release.

中文翻译:

通过物理化学性质和相互作用能探讨了抗癌药物5-氟尿嘧啶在胶束介质中的分配:定量研究在药物输送中的意义。

诸如胶束,囊泡和其他纳米乳剂之类的药物输送载体对于增强药物在体内的生物利用度是必不可少的。我们已经测量并关联了阴离子表面活性剂十二烷基硫酸钠胶束中的抗癌药物5-氟尿嘧啶的理化性质。阳离子表面活性剂十六烷基三甲基溴化铵,与非离子表面活性剂triton X-100具有高能相互作用。已经根据强度,性质和分配程度解释了伴随着将药物分配到表面活性剂胶束中的热力学特征以及从水转移到胶束的标准部分摩尔体积和标准部分摩尔可压缩性。已经确定了负责胶束相互作用/分配的药物上的官能团。5-氟尿嘧啶在两个或三个顺序分配行为中的相互作用取决于表面活性剂胶束的性质,使得能够对分配过程进行详细的机理分析。已经解决了结构-属性-能量关系,以获取对药物和胶束之间相互作用本质的更深入了解。此类研究提供了有关药物分子上官能团重要性的信息,可以对其进行修饰,以在药物输送载体中实现最佳分配,从而解决有效的靶向释放问题。已经解决了结构-属性-能量关系,以获取对药物和胶束之间相互作用本质的更深入了解。此类研究提供了有关药物分子上官能团重要性的信息,可以对其进行修饰,以在药物输送载体中实现最佳分配,从而解决有效的靶向释放问题。已经解决了结构-属性-能量关系,以获取对药物和胶束之间相互作用本质的更深入了解。此类研究提供了有关药物分子上官能团重要性的信息,可以对其进行修饰,以在药物输送载体中实现最佳分配,从而解决有效的靶向释放问题。
更新日期:2019-12-31
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