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Bifunctional Dendritic Structures Based on AB2C Monomers

机译:基于AB2C单体的双官能树枝状结构

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Dendrimers, compared to linear polymers, offers many unique complimentary properties and therefore gained increased interest. Much attention is directed to biological applications including: gene delivery agents, anticancer therapeutics, antiviral therapeutics, protein mimics, contrast agents for imaging and diagnostics.Dendrimers unique properties are associated to their composition, which consists of three parts: the core, internal branching and periphery. Traditionally, dendrimers are synthesized in repetitive fashion using ABx monomers that are radially connected from a multifunctional core. The resulted dendrimers are monodispersed, nano size, structures with inactive interior and multiple functional groups at the periphery. The high density of functional groups at the exterior is ideal in applications where improved sensitivity is important, for example in contrast imaging, diagnostics and multivalent interaction events Moreover, the structural cavities surrounding the core can be used to entrap drugs inside the dendrimers for in-vivo delivery purposes. Consequently, dendrimers can prolong the circulation time of drugs in the blood, decrease the toxicity, and increase the solubility of entrapped drugs. The latter is an important property of dendrimers since forty percent of all active pharmaceutical ingredients (APIs) fails in development due to poor water solubility. Furthermore, dendrimers confined structure is suitable for drug delivery since the Enhanced Permeability and Retention (EPR) effect is highly desirable in cancer treatments. In fact, the flawless structure of dendrimers has shown to be important in enhancing its ability to cross the cell membrane.3 Recent advancement in dendrimer synthesis, has allowed the construction of more elegant dendritic structures in which the internal and external structure can efficiently be tailored.
机译:与线性聚合物相比,树枝状大分子提供许多独特的互补性,因此获得了增加的兴趣。众多关注涉及生物学应用,包括:基因递送剂,抗癌治疗剂,抗病毒治疗剂,蛋白质模拟物,用于成像和诊断的造影剂.Denders独特的性质与其组合物相关,其组成三个部分:核心,内部分支和周边。传统上,使用从多功能芯径向连接的ABX单体以重复方式合成树枝状过敏率。由此产生的树枝状大分子是单分散的,纳米尺寸,具有无活性内部的结构和周边的多个官能团。外部的官能团的高密度是在改进的灵敏度重要的应用中的理想选择,例如在对比度成像,诊断和多价相互作用事件中,围绕芯的结构腔可用于捕获树枝内部的药物体内交付目的。因此,树枝状大分子可以延长血液中药物的循环时间,降低毒性,并增加斑点药物的溶解度。后者是树枝状大分子的重要特征,因为由于水溶解性差,所有活性药物成分(API)的百分之四十百分之均未发生开发。此外,树枝状大分子限制结构适用于药物递送,因为在癌症治疗中非常需要增强的渗透性和保留(EPR)效应。事实上,树枝状大分子的无瑕结构已经表明在提高其交叉细胞膜的能力方面是重要的,这是树枝状过敏器合成的最新进步,允许建造更优雅的树突结构,其中内部和外部结构可以有效地定制。

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