Designing macromolecules for therapeutic applications:: Polyester dendrimer-poly(ethylene oxide) "bow-tie" hybrids with tunable molecular weight and architecture
Designing macromolecules for therapeutic applications:: Polyester dendrimer-poly(ethylene oxide) "bow-tie" hybrids with tunable molecular weight and architecture
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DOI：
10.1021/ja028100n
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发表时间：
2002-11-27
影响因子：
15
通讯作者：
Fréchet, JMJ
中科院分区：
文献类型：
--
作者：
Gillies, ER;Fréchet, JMJ
描述了用于药物输送和相关治疗应用的新型聚酯树枝状聚合物、聚环氧乙烷杂化系统的设计和制备，这些系统由两个共价连接的聚酯树枝状分子组成，其中一个树枝状分子提供用于连接治疗活性部分的多种功能手柄，而另一个用于连接增溶性聚环氧乙烷链。通过改变树枝状分子的生成和聚环氧乙烷链的质量，可以容易地控制分子量、结构和载药量。使用会聚和发散方法合成“领结”形状的树突支架，在两个树突的外围具有正交保护基团。然后使用有效的偶联程序将聚环氧乙烷连接到一根树枝的外围。制备了一个由八种分子量范围为约 20 kDa 至 160 kDa 的载体组成的小型文库，并通过各种技术进行了表征，确认了它们明确的结构。
The design and preparation of new polyester dendrimer, poly(ethylene oxide) hybrid systems for drug delivery and related therapeutic applications, are described, These systems consist of two covalently attached polyester dendrons, where one dendron provides multiple functional handles for the attachment of therapeutically active moieties, while the other is used for attachment of solubilizing poly(ethylene oxide) chains. By varying the generation of the dendrons and the mass of the poly(ethylene oxide) chains, the molecular weight, architecture, and drug loading can be readily controlled. The "bow-tie" shaped dendritic scaffold was synthesized using both convergent and divergent methods, with orthogonal protecting groups on the periphery of the two dendrons. Poly(ethylene oxide) was then attached to the periphery of one dendron using an efficient coupling procedure. A small library of eight carriers with molecular weights ranging from about 20 kDa to 160 kDa were prepared and characterized by various techniques, confirming their well-defined structures.