Multifunctional polymeric nanoparticles from diverse bioactive agents

Multifunctional polymeric nanoparticles from diverse bioactive agents
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DOI:
10.1021/ja056378k
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发表时间:
2006-04-05
影响因子:
15
通讯作者:
Nguyen, ST
Nguyen, ST
中科院分区:
化学1区
文献类型:
--
作者:
Bertin, PA;Gibbs, JM;Nguyen, ST

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我们提出了一种合理的方法,将多种生物活性物质,如DNA、蛋白质和药物分子组装成核-壳多功能聚合物纳米粒子(PNPs),可以内化在人乳腺癌细胞中。利用开环复分解聚合(ROMP),制备了含有小分子药物片段(>50% w/w)和甲基化六甘醇片段的嵌段共聚物,并将其组装成PNPs,允许单链DNA序列和/或肿瘤靶向抗体的表面偶联。由此产生的抗体功能化颗粒很容易被过度表达相应抗原的乳腺癌细胞所吸收。
We present a rational approach for assembling diverse bioactive agents, such as DNA, proteins, and drug molecules, into core−shell multifunctional polymeric nanoparticles (PNPs) that can be internalized in human breast cancer cells. Using ring-opening metathesis polymerization (ROMP), block copolymers containing small-molecule drug segments (>50% w/w) and tosylated hexaethylene glycol segments were prepared and assembled into PNPs that allowed for the surface conjugation of single-stranded DNA sequences and/or tumor-targeting antibodies. The resulting antibody-functionalized particles were readily uptaken by breast cancer cells that overexpressed the corresponding antigens.