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首页> 外文期刊>Chemistry: A European journal >Water-Soluble Dendritic Core-Shell-Type Architectures Based on Polyglycerol for Solubilization of Hydrophobic Drugs
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Water-Soluble Dendritic Core-Shell-Type Architectures Based on Polyglycerol for Solubilization of Hydrophobic Drugs

机译：基于聚甘油的水溶性树突核壳型体系结构对疏水性药物的增溶作用

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摘要

Since many potential drugs are poorly water soluble,there is a high demand for solubilization agents.Here,we describe the synthesis of den dritic core-shell-type architectures based on hyperbranched polyglycerol for the solubilization of hydrophobic drugs.Amphiphilic macromolecules containing hydrophobic biphenyl groups in the core were synthesized in an efficient three-or four-step proce dure by employing Suzuki-coupling re actions.These species were then used to solubilize the commercial drug ni-modipine,a calcium antagonist used for the treatment of heart diseases and neurological deficits.Pyrene was also used as a hydrophobic model com pound.It turned out that the transport properties of the dendritic polyglycerol derivatives,which are based on hydro phobic host-guest interactions,depend strongly on the degree and type of core functionalization.In the case of the multifunctional nimodipine,additional specific polymer-drug interactions could be tailored by this flexible core design,as detected by UV spectrosco py.The enhancement of solubilization increased 300-fold for nimodipine and 6000-fold for pyrene at a polymer con centration of 10 wt%.The sizes of the polymer-drug complexes were deter mined by both dynamic light scattering(DLS)experiments and transmission electron microscopy(TEM),and ex tremely well-defined aggregates with diameters of approximately 10 nm in the presence of a drug were observed.These findings together with a low crit ical aggregate concentration of 4×10~(-6)molL-1 indicate the controlled self-assembly of the presented amphi philic dendritic core-shell-type archi tectures rather than a unimolecular transport behavior.
机译：由于许多潜在的药物难溶于水，因此对增溶剂的需求很高。在此，我们描述了基于超支化聚甘油的树突状核-壳型结构的合成，用于增溶疏水性药物。含有疏水性联苯基的两亲大分子通过使用Suzuki偶联反应，以高效的三步或四步过程合成了核心化合物，然后将这些物质用于溶解商品药物ni-modipine，这是一种用于治疗心脏病和神经系统疾病的钙拮抗剂also还被用作疏水性模型化合物。事实证明，基于疏水性主客体相互作用的树突状聚甘油衍生物的转运特性在很大程度上取决于核心功能化的程度和类型。在多功能尼莫地平的情况下，可以通过这种灵活的核心设计来定制其他特定的聚合物-药物相互作用，紫外分光光度法测定聚合物浓度为10 wt％时，尼莫地平的增溶作用增加300倍，pyr的增溶作用增加6000倍。聚合物-药物复合物的大小由两种动态光散射确定（观察了DLS）和透射电镜（TEM）的存在，观察到在药物存在下直径约10 nm的极其明确的聚集体，这些发现以及临界聚集体浓度低至4×10〜（- 6）molL-1表示所提出的两亲树突状核壳型结构的受控自组装，而不是单分子的运输行为。

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