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Bicomponent polymeric micelles for pH-controlled delivery of doxorubicin.
Drug Delivery ( IF 6 ) Pub Date : 2020-02-24 , DOI: 10.1080/10717544.2020.1726526
Chunyun Wang 1 , Peilan Qi 1 , Yan Lu 1 , Lei Liu 1 , Yanan Zhang 1 , Qianli Sheng 1 , Tianshun Wang 1 , Mengying Zhang 1 , Rui Wang 1 , Shiyong Song 1
Affiliation  

Stimuli-responsive drug delivery systems (DDSs) are expected to realize site-specific drug release and kill cancer cells selectively. In this study, a pH-responsive micelle was designed utilizing the pH-sensitivity of borate bonds formed between dopamine and boronic acid. First, methyl (polyethylene glycol)-block-polycaprolactone (mPEG-PCL) was conjugated with 4-cyano-4-(thiobenzoylthio)pentanoic acid (CTP) to obtain a macroinitiator. Two different segments poly(dopamine methacrylamide) (PDMA) and poly(vinylphenylboronic acid) (PVBA) were then grafted to the end of mPEG-PCL. Two triblock copolymers, mPEG-PCL-PDMA and mPEG-PCL-PVBA, were then obtained by reversible addition-fragmentation transfer (RAFT) polymerization. These copolymers and their mixture self-assembled in aqueous solution to form micelles that were able to load hydrophobic anticancer drug doxorubicin (DOX). These two-component micelles were found to be pH-sensitive, in contrast to the one-component micelles. Furthermore, MTT studies showed that the micelles were almost nontoxic. The DOX-loaded micelles showed cytotoxicity equivalent to that of DOX at high concentration. In vivo antitumor experiments showed that this pH-sensitive polymeric micellar system had an enhanced therapeutic effect on tumors. These two-component boronate-based pH micelles are universally applicable to the delivery of anticancer drugs, showing great potential for cancer therapy.

中文翻译:

pH控制的阿霉素双组分聚合胶束。

刺激反应性药物递送系统(DDS)有望实现特定部位的药物释放并选择性杀死癌细胞。在这项研究中,利用多巴胺和硼酸之间形成的硼酸酯键的pH敏感性设计了一种pH响应胶束。首先,将甲基(聚乙二醇)-嵌段-聚己内酯(mPEG-PCL)与4-氰基-4-(硫代苯甲酰基硫基)戊酸(CTP)缀合以获得大分子引发剂。然后将两个不同的片段聚(多巴胺甲基丙烯酰胺)(PDMA)和聚(乙烯基苯基硼酸)(PVBA)接枝到mPEG-PCL的末端。然后通过可逆的加成-断裂转移(RAFT)聚合获得两种三嵌段共聚物,mPEG-PCL-PDMA和mPEG-PCL-PVBA。这些共聚物及其混合物在水溶液中自组装形成能负载疏水性抗癌药阿霉素(DOX)的胶束。与单组分胶束相反,发现这些二组分胶束对pH敏感。此外,MTT研究表明,胶束几乎无毒。载有DOX的胶束显示出与高浓度DOX相同的细胞毒性。体内抗肿瘤实验表明,这种对pH敏感的聚合物胶束系统对肿瘤具有增强的治疗作用。这些基于硼酸酯的两组分pH胶束普遍适用于抗癌药物的输送,显示出巨大的癌症治疗潜力。MTT研究表明,胶束几乎无毒。载有DOX的胶束显示出与高浓度DOX相同的细胞毒性。体内抗肿瘤实验表明,这种对pH敏感的聚合物胶束系统对肿瘤具有增强的治疗作用。这些基于硼酸酯的两组分pH胶束普遍适用于抗癌药物的输送,显示出巨大的癌症治疗潜力。MTT研究表明,胶束几乎无毒。载有DOX的胶束显示出与高浓度DOX相同的细胞毒性。体内抗肿瘤实验表明,这种对pH敏感的聚合物胶束系统对肿瘤具有增强的治疗作用。这些基于硼酸酯的两组分pH胶束普遍适用于抗癌药物的输送,显示出巨大的癌症治疗潜力。
更新日期:2020-04-20
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