Cyclic Peptide–Polymer Nanotubes as Efficient and Highly Potent Drug Delivery Systems for Organometallic Anticancer Complexes,Biomacromolecules

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Cyclic Peptide–Polymer Nanotubes as Efficient and Highly Potent Drug Delivery Systems for Organometallic Anticancer Complexes
Biomacromolecules ( IF 5.5 ) Pub Date : 2017-12-14 00:00:00 , DOI: 10.1021/acs.biomac.7b01491
Sophie C Larnaudie ₁ , Johannes C Brendel _{1,

2} , Isolda Romero-Canelón ₁ , Carlos Sanchez-Cano ₁ , Sylvain Catrouillet ₃ , Joaquin Sanchis ₂ , James P C Coverdale ₁ , Ji-Inn Song ₁ , Abraha Habtemariam ₁ , Peter J Sadler ₁ , Katrina A Jolliffe ₄ , Sébastien Perrier _{1,

2,

5}

Affiliation

Functional drug carrier systems have potential for increasing solubility and potency of drugs while reducing side effects. Complex polymeric materials, particularly anisotropic structures, are especially attractive due to their long circulation times. Here, we have conjugated cyclic peptides to the biocompatible polymer poly(2-hydroxypropyl methacrylamide) (pHPMA). The resulting conjugates were functionalized with organoiridium anticancer complexes. Small angle neutron scattering and static light scattering confirmed their self-assembly and elongated cylindrical shape. Drug-loaded nanotubes exhibited more potent antiproliferative activity toward human cancer cells than either free drug or the drug-loaded polymers, while the nanotubes themselves were nontoxic. Cellular accumulation studies revealed that the increased potency of the conjugate appears to be related to a more efficient mode of action rather than a higher cellular accumulation of iridium.

中文翻译：

环状肽-聚合物纳米管作为有机金属抗癌复合物的高效高效药物递送系统

功能性药物载体系统具有增加药物溶解度和效力同时减少副作用的潜力。复杂的聚合材料，特别是各向异性结构，由于其长循环时间而特别有吸引力。在这里，我们将环状肽与生物相容性聚合物聚 (2-羟丙基甲基丙烯酰胺) (pHPMA) 结合在一起。所得缀合物用有机铱抗癌复合物官能化。小角度中子散射和静态光散射证实了它们的自组装和细长的圆柱形状。与游离药物或载药聚合物相比，载药纳米管对人类癌细胞表现出更有效的抗增殖活性，而纳米管本身是无毒的。

更新日期：2017-12-14

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