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首页> 外文期刊>Biomacromolecules >PAMAM Dendrimer-Based Multifunctional Conjugate for Cancer Therapy:Synthesis,Characterization,and Functionality
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PAMAM Dendrimer-Based Multifunctional Conjugate for Cancer Therapy:Synthesis,Characterization,and Functionality

机译：基于PAMAM树状聚合物的多功能偶联物，用于癌症治疗：合成，表征和功能

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摘要

Poly(amidoamine) (PAMAM) dendrimer-based multifunctional cancer therapeutic conjugates have been designed and synthesized.The primary amino groups on the surface of the generation 5 (G5) PAMAM dendrimer were neutralized through partial acetylation,providing enhanced solubility of the dendrimer (in conjugation of FITC (fluorescein isothiocyanate)) and preventing nonspecific targeting interactions (in vitro and in vivo) during delivery.The functional molecules fluorescein isothiocyanate (FITC,an imaging agent),folic acid (FA,targets overexpressed folate receptors on specific cancer cells),and paclitaxel (taxol,a chemotherapeutic drug) were conjugated to the remaining nonacetylated primary amino groups.The appropriate control dendrimer conjugates have been synthesized as well.Characterization of the G5 PAMAM dendrimer and its nanosize conjugates,including the molecular weight and number of primary amine groups,has been determined by multiple analytical methods such as gel permeation chromatography (GPC),nuclear magnetic resonance spectroscopy (NMR),potentiometric titration,high-performance liquid chromatography (HPLC),and UV spectroscopy.These multifunctional dendrimer conjugates have been tested in vitro for targeted delivery of chemotherapeutic and imaging agents to specific cancer cells.We present here the synthesis,characterization,and functionality of these dendrimer conjugates.
机译：设计并合成了基于聚（酰胺基胺）（PAMAM）树状大分子的多功能癌症治疗共轭物。第5代（G5）PAMAM树状大分子表面的伯氨基通过部分乙酰化被中和，从而提高了树状大分子的溶解性（在结合FITC（异硫氰酸荧光素）并防止分娩过程中的非特异性靶向相互作用（体外和体内）功能分子异硫氰酸荧光素（成像剂），叶酸（FA，靶向特定癌细胞上过量表达的叶酸受体）然后将紫杉醇（紫杉醇，一种化疗药物）与其余未乙酰化的伯氨基偶联。还合成了合适的对照树枝状聚合物偶联物。G5PAMAM树枝状聚合物及其纳米级偶联物的表征，包括分子量和一级伯胺基已通过多种分析方法测定，例如凝胶渗透色谱质谱（GPC），核磁共振波谱（NMR），电位滴定，高效液相色谱（HPLC）和紫外光谱。这些多功能树状聚合物偶联物已在体外进行了测试，可将化疗药物和成像剂定向递送至特定癌细胞我们在这里介绍了这些树枝状大分子共轭物的合成，表征和功能。

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