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Micelles with a Loose Core Self‐Assembled from Coil‐g‐Rod Graft Copolymers Displaying High Drug Loading Capacity
Macromolecular Chemistry and Physics ( IF 2.5 ) Pub Date : 2020-05-27 , DOI: 10.1002/macp.202000121 Qijing Huang 1 , Zhanwen Xu 1 , Chunhua Cai 1 , Jiaping Lin 1
Macromolecular Chemistry and Physics ( IF 2.5 ) Pub Date : 2020-05-27 , DOI: 10.1002/macp.202000121 Qijing Huang 1 , Zhanwen Xu 1 , Chunhua Cai 1 , Jiaping Lin 1
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High drug loading capacity is one of the critical demands of micellar drug‐delivery vehicles; however, it is a challenging work. Herein, it is demonstrated that micelles self‐assembled from poly(ethylene glycol)‐graft‐poly(γ‐benzyl‐l‐glutamate) (PEG‐g‐PBLG) coil‐g‐rod graft copolymers display high drug‐loading capacity for doxorubicin (DOX) model drugs. As revealed by a combination study of experiments and dissipative particle dynamics simulations, the high drug‐loading capacity of the micelles is related to the loose core structure of the micelles. In these micelles, the hydrophobic PBLG grafts randomly disperse in the micelle core due to their rigid nature and the coil‐g‐rod topology of the graft copolymers, which results in a loose core of the micelles. The structure of the graft copolymer, including the length of rod grafts, the length of coil backbone, and the grafting ratio of the rod grafts affecting the arrangement of the rod grafts in the micelle core has influence on the drug‐loading capacity of the micelles. Besides, the strong π–π stacking interaction between graft copolymers and DOX also plays an important part in achieving high drug‐loading capacity. In vitro studies reveal that these drug‐loaded micelles show good biocompatibility, and the DOX can be gradually released from the micelles.
中文翻译：
用高载量的Coil-g-Rod接枝共聚物自组装的纤芯松散胶束
高载药量是胶束输送工具的关键要求之一。但是，这是一项具有挑战性的工作。本文中，证明从聚（乙二醇），该胶束自组装-接枝的聚（γ苄基升-谷氨酸）（PEG-克-PBLG）coil-克-ROD接枝共聚物显示出高的药物负载能力为阿霉素（DOX）模型药物。正如实验和耗散粒子动力学模拟的组合研究所揭示的那样，胶束的高载药量与胶束的松散核心结构有关。在这些胶束中，疏水PBLG移植物在胶束芯中随机分散的，由于其刚性的性质和coil-克接枝共聚物的杆状拓扑结构，导致胶束的核心松散。接枝共聚物的结构，包括棒状接枝的长度，线圈骨架的长度以及棒状接枝的接枝率，影响棒状接枝在胶束芯中的排列，对胶束的载药量有影响。 。此外，接枝共聚物与DOX之间强烈的π-π堆积相互作用在实现高载药量方面也起着重要作用。体外研究表明，这些载药胶束具有良好的生物相容性，DOX可以逐渐从胶束中释放出来。
更新日期：2020-05-27
中文翻译：
用高载量的Coil-g-Rod接枝共聚物自组装的纤芯松散胶束
高载药量是胶束输送工具的关键要求之一。但是，这是一项具有挑战性的工作。本文中，证明从聚（乙二醇），该胶束自组装-接枝的聚（γ苄基升-谷氨酸）（PEG-克-PBLG）coil-克-ROD接枝共聚物显示出高的药物负载能力为阿霉素（DOX）模型药物。正如实验和耗散粒子动力学模拟的组合研究所揭示的那样，胶束的高载药量与胶束的松散核心结构有关。在这些胶束中，疏水PBLG移植物在胶束芯中随机分散的，由于其刚性的性质和coil-克接枝共聚物的杆状拓扑结构，导致胶束的核心松散。接枝共聚物的结构，包括棒状接枝的长度，线圈骨架的长度以及棒状接枝的接枝率，影响棒状接枝在胶束芯中的排列，对胶束的载药量有影响。 。此外，接枝共聚物与DOX之间强烈的π-π堆积相互作用在实现高载药量方面也起着重要作用。体外研究表明，这些载药胶束具有良好的生物相容性，DOX可以逐渐从胶束中释放出来。
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