PDF(Pubmed)
Abstract：
Cationic dendritic amphiphiles were prepared through the linkage of interesting hydrophobic molecules such as cholesterol or vitamin E to the focal point of carbosilane dendrons. These new dendritic systems self-assembled in saline, producing micellar aggregates with hydrodynamic diameters ranging from 6.5 to 9.2 nm, and critical micelle concentrations of approximately 5 and 10 μM for second- and third-generation systems, respectively. The assemblies were able to encapsulate drugs of different charges (anionic, neutral, and cationic). Surprisingly, a 92% encapsulation efficiency for diclofenac was achieved in micelles prepared from second-generation dendrons. Toxicity measurements on peripheral blood mononuclear cells indicated different behavior depending on the generation, corresponding to the micellar regime. In contrast to the third-generation system, the second-generation system was non-toxic up to 20 μM, opening a window for its use in a micellar regimen, thereby operating as a drug delivery system for different biomedical applications.
摘要：
阳离子树枝状两亲物是通过将感兴趣的疏水分子如胆固醇或维生素E连接到碳硅烷树枝状物的焦点上来制备的。这些新的树枝状系统在盐水中自组装，产生流体动力学直径为6.5至9.2nm的胶束聚集体，第二代和第三代系统的临界胶束浓度约为5和10μM，分别。组件能够封装不同电荷的药物（阴离子，中性,和阳离子）。令人惊讶的是,在由第二代树突制备的胶束中，双氯芬酸的包封率为92％。对外周血单核细胞的毒性测量表明不同的行为取决于世代，对应于胶束体系。与第三代系统相比，第二代系统的毒性高达20μM，打开一个窗口，用于胶束方案，从而作为用于不同生物医学应用的药物递送系统。
