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Amphiphilic siRNA Conjugates for Co-Delivery of Nucleic Acids and Hydrophobic Drugs
Bioconjugate Chemistry ( IF 4.0 ) Pub Date : 2017-07-26 00:00:00 , DOI: 10.1021/acs.bioconjchem.7b00222 Soo Hyeon Lee 1 , Jeong Yu Lee 2 , Jee Seon Kim 3 , Tae Gwan Park 4 , Hyejung Mok 5
Bioconjugate Chemistry ( IF 4.0 ) Pub Date : 2017-07-26 00:00:00 , DOI: 10.1021/acs.bioconjchem.7b00222 Soo Hyeon Lee 1 , Jeong Yu Lee 2 , Jee Seon Kim 3 , Tae Gwan Park 4 , Hyejung Mok 5
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Combination therapy of nucleic acids and chemical drugs for cancer treatment is a promising strategy to enhance the therapeutic efficacy by simultaneously regulating multiple troublesome pathways. In this study, we report on polyethylene glycol-siRNA-polycaprolactone (PEG-siRNA-PCL) micelles that encapsulate hydrophobic drugs for efficient co-delivery of siRNA and drugs to cancer cells. Amphiphilic PEG-siRNA-PCL copolymers were synthesized by annealing antisense siRNA-PCL conjugates with sense siRNA-PEG conjugates. After paclitaxel encapsulation, PEG-siRNA-PCL micelles containing antiapoptotic Bcl-2-specific siRNA were stabilized with linear polyethylenimine via electrostatic interactions. Stabilized PEG-siRNA-PCL micelles showed superior anticancer effects, assessed by caspase-3 activity analysis, apoptotic cell staining, and a cytotoxicity test, to those of paclitaxel-free PEG-siRNA-PCL micelles and unmodified siRNAs. The strong anticancer activity of paclitaxel-incorporated siRNA micelles can be attributed to the synergistic effect of Bcl-2 siRNA and paclitaxel. This work provides an efficient co-delivery platform for combination anticancer therapy with siRNA and chemotherapy.
中文翻译：
两亲性siRNA结合用于核酸和疏水性药物的共同递送
核酸和化学药物的联合疗法用于癌症治疗是一种有前景的策略，可通过同时调节多种麻烦的途径来提高治疗效果。在这项研究中，我们报道了聚乙二醇-siRNA-聚己内酯（PEG-siRNA-PCL）胶束，该胶束封装了疏水性药物，可将siRNA和药物有效地共同递送至癌细胞。通过使反义siRNA-PCL缀合物与有义siRNA-PEG缀合物退火来合成两亲性PEG-siRNA-PCL共聚物。紫杉醇包封后，通过线性相互作用通过线性聚乙烯亚胺稳定含有抗凋亡Bcl-2特异性siRNA的PEG-siRNA-PCL胶束。经caspase-3活性分析，凋亡细胞染色和细胞毒性试验评估，稳定的PEG-siRNA-PCL胶束表现出优异的抗癌作用，不含紫杉醇的PEG-siRNA-PCL胶束和未修饰的siRNA。掺入紫杉醇的siRNA胶束具有很强的抗癌活性，这可归因于Bcl-2 siRNA与紫杉醇的协同作用。这项工作为siRNA与化学疗法联合抗癌治疗提供了有效的共同交付平台。
更新日期：2017-07-28
中文翻译：
两亲性siRNA结合用于核酸和疏水性药物的共同递送
核酸和化学药物的联合疗法用于癌症治疗是一种有前景的策略，可通过同时调节多种麻烦的途径来提高治疗效果。在这项研究中，我们报道了聚乙二醇-siRNA-聚己内酯（PEG-siRNA-PCL）胶束，该胶束封装了疏水性药物，可将siRNA和药物有效地共同递送至癌细胞。通过使反义siRNA-PCL缀合物与有义siRNA-PEG缀合物退火来合成两亲性PEG-siRNA-PCL共聚物。紫杉醇包封后，通过线性相互作用通过线性聚乙烯亚胺稳定含有抗凋亡Bcl-2特异性siRNA的PEG-siRNA-PCL胶束。经caspase-3活性分析，凋亡细胞染色和细胞毒性试验评估，稳定的PEG-siRNA-PCL胶束表现出优异的抗癌作用，不含紫杉醇的PEG-siRNA-PCL胶束和未修饰的siRNA。掺入紫杉醇的siRNA胶束具有很强的抗癌活性，这可归因于Bcl-2 siRNA与紫杉醇的协同作用。这项工作为siRNA与化学疗法联合抗癌治疗提供了有效的共同交付平台。
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