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Combination Chemotherapy of Lung Cancer - Co-Delivery of Docetaxel Prodrug and Cisplatin Using Aptamer-Decorated Lipid-Polymer Hybrid Nanoparticles.
Drug Design, Development and Therapy ( IF 4.7 ) Pub Date : 2020-06-09 , DOI: 10.2147/dddt.s246574 Ruifeng Wu 1 , Zhiqiang Zhang 1 , Baohua Wang 2 , Ge Chen 3 , Yaozhong Zhang 3 , Haowen Deng 3 , Zilong Tang 3 , Junjie Mao 3 , Lei Wang 3
Drug Design, Development and Therapy ( IF 4.7 ) Pub Date : 2020-06-09 , DOI: 10.2147/dddt.s246574 Ruifeng Wu 1 , Zhiqiang Zhang 1 , Baohua Wang 2 , Ge Chen 3 , Yaozhong Zhang 3 , Haowen Deng 3 , Zilong Tang 3 , Junjie Mao 3 , Lei Wang 3
Affiliation
Purpose: Lung cancer is the leading cause of cancer mortality worldwide. Drug resistance is the major barrier for the treatment of non-small cell lung cancer (NSCLC). The aim of this research is to develop an aptamer-decorated hybrid nanoparticle for the co-delivery of docetaxel prodrug (DTXp) and cisplatin (DDP) and to treat lung cancer.
Materials and Methods: Aptamer-conjugated lipid–polymer ligands and redox-sensitive docetaxel prodrug were synthesized. DTXp and DDP were loaded into the lipid–polymer hybrid nanoparticles (LPHNs). The targeted efficiency of aptamer-decorated, DTXp and DDP co-encapsulated LPHNs (APT-DTXp/DDP-LPHNs) was determined by performing a cell uptake assay by flow cytometry-based analysis. In vivo biodistribution and anticancer efficiency of APT-DTXp/DDP-LPHNs were evaluated on NSCLC-bearing mice xenograft.
Results: APT-DTXp/DDP-LPHNs had a particle size of 213.5 ± 5.3 nm, with a zeta potential of 15.9 ± 1.9 mV. APT-DTXp/DDP-LPHNs exhibited a significantly enhanced cytotoxicity (drug concentration causing 50% inhibition was 0.71 ± 0.09 μg/mL), synergy antitumor effect (combination index was 0.62), and profound tumor inhibition ability (tumor inhibition ratio of 81.4%) compared with the non-aptamer-decorated LPHNs and single drug-loaded LPHNs.
Conclusion: Since the synergistic effect of the drugs was found in this system, it would have great potential to inhibit lung tumor cells and in vivo tumor growth.
Keywords: lung cancer, combination therapy, docetaxel prodrug, cisplatin, aptamer-decorated, lipid–polymer hybrid nanoparticles
中文翻译：
肺癌的联合化疗 - 使用适配体修饰的脂质-聚合物混合纳米颗粒共同递送多西紫杉醇前药和顺铂。
目的：肺癌是全球癌症死亡的主要原因。耐药性是治疗非小细胞肺癌（NSCLC）的主要障碍。这项研究的目的是开发一种适配体修饰的混合纳米颗粒，用于多西他赛前药 (DTXp) 和顺铂 (DDP) 的共同递送并治疗肺癌。
材料和方法：合成了适体缀合的脂质聚合物配体和氧化还原敏感的多西紫杉醇前药。DTXp 和 DDP 被加载到脂质-聚合物混合纳米粒子 (LPHN) 中。适配体修饰的 DTXp 和 DDP 共封装 LPHN (APT-DTXp/DDP-LPHN) 的靶向效率通过基于流式细胞术的分析进行细胞摄取测定来确定。在携带 NSCLC 的小鼠异种移植物上评估 APT-DTXp/DDP-LPHN 的体内生物分布和抗癌效率。
结果：APT-DTXp/DDP-LPHN 的粒径为 213.5 ± 5.3 nm，zeta 电位为 15.9 ± 1.9 mV。APT-DTXp/DDP-LPHNs表现出显着增强的细胞毒性（引起50%抑制的药物浓度为0.71±0.09 μg/mL）、协同抗肿瘤作用（组合指数为0.62）和显着的肿瘤抑制能力（肿瘤抑制率为81.4% ) 与非适配体修饰的 LPHN 和单载药 LPHN 相比。
结论：由于在该系统中发现了药物的协同作用，在抑制肺肿瘤细胞和体内肿瘤生长方面具有很大的潜力。
关键词：肺癌，联合治疗，多西他赛前药，顺铂，适配体修饰，脂质-聚合物杂化纳米粒子
更新日期：2020-06-09
Materials and Methods: Aptamer-conjugated lipid–polymer ligands and redox-sensitive docetaxel prodrug were synthesized. DTXp and DDP were loaded into the lipid–polymer hybrid nanoparticles (LPHNs). The targeted efficiency of aptamer-decorated, DTXp and DDP co-encapsulated LPHNs (APT-DTXp/DDP-LPHNs) was determined by performing a cell uptake assay by flow cytometry-based analysis. In vivo biodistribution and anticancer efficiency of APT-DTXp/DDP-LPHNs were evaluated on NSCLC-bearing mice xenograft.
Results: APT-DTXp/DDP-LPHNs had a particle size of 213.5 ± 5.3 nm, with a zeta potential of 15.9 ± 1.9 mV. APT-DTXp/DDP-LPHNs exhibited a significantly enhanced cytotoxicity (drug concentration causing 50% inhibition was 0.71 ± 0.09 μg/mL), synergy antitumor effect (combination index was 0.62), and profound tumor inhibition ability (tumor inhibition ratio of 81.4%) compared with the non-aptamer-decorated LPHNs and single drug-loaded LPHNs.
Conclusion: Since the synergistic effect of the drugs was found in this system, it would have great potential to inhibit lung tumor cells and in vivo tumor growth.
Keywords: lung cancer, combination therapy, docetaxel prodrug, cisplatin, aptamer-decorated, lipid–polymer hybrid nanoparticles
中文翻译：
肺癌的联合化疗 - 使用适配体修饰的脂质-聚合物混合纳米颗粒共同递送多西紫杉醇前药和顺铂。
目的：肺癌是全球癌症死亡的主要原因。耐药性是治疗非小细胞肺癌（NSCLC）的主要障碍。这项研究的目的是开发一种适配体修饰的混合纳米颗粒，用于多西他赛前药 (DTXp) 和顺铂 (DDP) 的共同递送并治疗肺癌。
材料和方法：合成了适体缀合的脂质聚合物配体和氧化还原敏感的多西紫杉醇前药。DTXp 和 DDP 被加载到脂质-聚合物混合纳米粒子 (LPHN) 中。适配体修饰的 DTXp 和 DDP 共封装 LPHN (APT-DTXp/DDP-LPHN) 的靶向效率通过基于流式细胞术的分析进行细胞摄取测定来确定。在携带 NSCLC 的小鼠异种移植物上评估 APT-DTXp/DDP-LPHN 的体内生物分布和抗癌效率。
结果：APT-DTXp/DDP-LPHN 的粒径为 213.5 ± 5.3 nm，zeta 电位为 15.9 ± 1.9 mV。APT-DTXp/DDP-LPHNs表现出显着增强的细胞毒性（引起50%抑制的药物浓度为0.71±0.09 μg/mL）、协同抗肿瘤作用（组合指数为0.62）和显着的肿瘤抑制能力（肿瘤抑制率为81.4% ) 与非适配体修饰的 LPHN 和单载药 LPHN 相比。
结论：由于在该系统中发现了药物的协同作用，在抑制肺肿瘤细胞和体内肿瘤生长方面具有很大的潜力。
关键词：肺癌，联合治疗，多西他赛前药，顺铂，适配体修饰，脂质-聚合物杂化纳米粒子
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