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Rapid Polymer Conjugation Strategies for the Generation of pH-Responsive, Cancer Targeting, Polymeric Nanoparticles
Biomacromolecules ( IF 6.2 ) Pub Date : 2018-04-24 00:00:00 , DOI: 10.1021/acs.biomac.8b00309
Weishuo Li , Jin Geng , Helen Titmarsh 1 , Alicia Megia-Fernandez , Kev Dhaliwal , Margaret Frame 1 , Mark Bradley
Affiliation  

The combination of controlled living polymerization in association with rapid and highly efficient macromolecule conjugation strategies provides a powerful tool for the synthesis of novel polymeric materials. Here functional block copolymers were rapidly and quantitatively conjugated using an efficient reaction between polymers containing a phenolic group and the 4-phenyl-3H-1,2,4-triazole-3,5(4H)-dione (PTAD) moiety and used to generate nanoparticles that encapsulated drugs. pH responsive amphiphilic block copolymers, which self-assemble into nanoparticles, were fabricated using our novel polymer conjugation strategy with the resulting system designed to promote drug release within the acidic milieu of the cancer microenvironment. The conjugation strategy also enabled the direct tagging of the nanoparticles with a range of fluorophores, targeting assets, or both with cargo release demonstrated in cancer cells.

中文翻译:

用于产生pH响应,靶向癌症的聚合物纳米粒子的快速聚合物共轭策略。

受控的活性聚合与快速高效的大分子偶联策略相结合,为合成新型聚合物材料提供了强大的工具。在此,使用含酚基的聚合物与4-苯基-3 H -1,2,4-三唑-3,5(4 H-二酮(PTAD)部分,并用于生成包裹药物的纳米颗粒。使用我们新颖的聚合物共轭策略,可自动组装成pH值的两亲嵌段共聚物,并设计出能促进药物在癌症微环境的酸性环境中释放的系统。结合策略还使得能够使用一系列荧光团,靶向资产或两者同时用癌细胞中证明的货物释放来直接标记纳米颗粒。
更新日期:2018-04-24
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