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Phenylboronic acid-functionalized unimolecular micelles based on a star polyphosphoester random copolymer for tumor-targeted drug delivery
Polymer Chemistry ( IF 4.1 ) Pub Date : 2020/02/21 , DOI: 10.1039/d0py00008f Li Zhang 1, 2, 3, 4, 5 , Dongjian Shi 1, 2, 3, 4, 5 , Yunyun Gao 6, 7, 8 , Tianyang Zhou 1, 2, 3, 4, 5 , Mingqing Chen 1, 2, 3, 4, 5
Polymer Chemistry ( IF 4.1 ) Pub Date : 2020/02/21 , DOI: 10.1039/d0py00008f Li Zhang 1, 2, 3, 4, 5 , Dongjian Shi 1, 2, 3, 4, 5 , Yunyun Gao 6, 7, 8 , Tianyang Zhou 1, 2, 3, 4, 5 , Mingqing Chen 1, 2, 3, 4, 5
Affiliation
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To overcome the thermodynamic instability of polymeric micelles in an extremely high dilution bio-environment, unimolecular micelles with covalently-bound molecular architectures have been widely studied for drug delivery. In this work, an amphiphilic multi-arm star random copolymer, polyamidoamine-poly(butenyl phospholane-co-methoxy phospholane) with phenylboronic acid end groups (abbreviated as PAMAM-P(BEP-co-MP)-PBA), was synthesized by a simple one-pot ring-opening polymerization with the fourth-generation PAMAM dendrimer as a macro-initiator. Then, unimolecular micelles (UMs) were formed by the obtained copolymers in a dilute aqueous solution. Dynamic light scattering (DLS) and transmission electron microscopy (TEM) results showed that the UMs possess uniform spherical structures and stable hydrodynamic sizes (ca. 20 nm). Besides, further information on polymer repeat unit numbers could be theoretically calculated by comparison of hydrodynamic sizes and contour lengths. Doxorubicin (DOX) could be encapsulated into the inner hydrophobic regions of the UMs. The obtained DOX-loaded UMs exhibited a slow and sustainable release behavior in an intracellular simulated environment. Furthermore, in vitro cytotoxicity and cellular uptake studies demonstrated that the DOX-loaded UMs could specifically recognize and accumulate in HepG2 cells, and then inhibit tumor cell growth effectively. Therefore, this PBA-functionalized unimolecular micelle could be a promising candidate for targeted drug delivery.
中文翻译：
基于星形聚磷酸酯无规共聚物的苯硼酸官能化的单分子胶束，用于靶向肿瘤的药物递送
为了克服聚合物胶束在极高稀释度的生物环境中的热力学不稳定性，已广泛研究了具有共价键合分子结构的单分子胶束用于药物递送。在这项工作中，两亲性多臂星形无规共聚物，聚酰氨基胺-聚（丁烯基phospholane-共-甲氧基磷杂环戊烷）与苯基酸端基（缩写为PAMAM-P（BEP-共-MP）-PBA），是通过简单的一锅开环聚合反应合成的，其中第四代PAMAM树状大分子为大分子引发剂。然后，由所得共聚物在稀水溶液中形成单分子胶束（UMs）。动态光散射（DLS）和透射电子显微镜（TEM）结果表明，UM具有均匀的球形结构和稳定的流体动力学尺寸（约20 nm）。此外，通过比较流体力学尺寸和轮廓长度，理论上可以计算出有关聚合物重复单元数的更多信息。阿霉素（DOX）可以封装在UM的内部疏水区域中。获得的装载DOX的UM在细胞内模拟环境中表现出缓慢且可持续的释放行为。此外，体外细胞毒性和细胞摄取研究表明，装载DOX的UMs可以特异性识别和积累在HepG2细胞中，然后有效抑制肿瘤细胞的生长。因此，这种PBA功能化的单分子胶束可能是靶向药物递送的有希望的候选者。
更新日期：2020-03-24
中文翻译：
基于星形聚磷酸酯无规共聚物的苯硼酸官能化的单分子胶束，用于靶向肿瘤的药物递送
为了克服聚合物胶束在极高稀释度的生物环境中的热力学不稳定性，已广泛研究了具有共价键合分子结构的单分子胶束用于药物递送。在这项工作中，两亲性多臂星形无规共聚物，聚酰氨基胺-聚（丁烯基phospholane-共-甲氧基磷杂环戊烷）与苯基酸端基（缩写为PAMAM-P（BEP-共-MP）-PBA），是通过简单的一锅开环聚合反应合成的，其中第四代PAMAM树状大分子为大分子引发剂。然后，由所得共聚物在稀水溶液中形成单分子胶束（UMs）。动态光散射（DLS）和透射电子显微镜（TEM）结果表明，UM具有均匀的球形结构和稳定的流体动力学尺寸（约20 nm）。此外，通过比较流体力学尺寸和轮廓长度，理论上可以计算出有关聚合物重复单元数的更多信息。阿霉素（DOX）可以封装在UM的内部疏水区域中。获得的装载DOX的UM在细胞内模拟环境中表现出缓慢且可持续的释放行为。此外，体外细胞毒性和细胞摄取研究表明，装载DOX的UMs可以特异性识别和积累在HepG2细胞中，然后有效抑制肿瘤细胞的生长。因此，这种PBA功能化的单分子胶束可能是靶向药物递送的有希望的候选者。
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