Shell‐Sheddable Poly(N‐2‐hydroxypropyl methacrylamide) Polymeric Micelles for Dual‐Sensitive Release of Doxorubicin,Macromolecular Rapid Communications

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Shell‐Sheddable Poly(N‐2‐hydroxypropyl methacrylamide) Polymeric Micelles for Dual‐Sensitive Release of Doxorubicin
Macromolecular Rapid Communications ( IF 4.2 ) Pub Date : 2018-05-16 , DOI: 10.1002/marc.201800139
Jiajing Zhang ₁ , Hao Tang ₂ , Yi Shen ₂ , Qingsong Yu ₂ , Zhihua Gan ₂

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Poly(ethylene glycol) (PEG) shell‐sheddable micelles are proved to be effective tools for rapid intracellular drug delivery. However, some adverse factors, such as the potential immunogenicity and the accelerated blood clearance, might be accompanied with the traditional PEG sheddable micelles. Here, a poly(N‐2‐hydroxypropyl methacrylamide) (PHPMA) sheddable block copolymer containing disulfide bonds on the main chain is prepared to form pH‐ and reduction‐dual‐responsive micelles. The most optimal synthetic route of the block copolymer is selected from three potential pathways. Doxorubicin is loaded via an acid‐labile hydrazone bond to achieve high drug loading content and to prevent premature drug release. As expected, as‐prepared shell‐sheddable micelles exhibit faster intracellular drug release and more satisfactory in vitro anticancer efficacy than the nonsheddable counterpart did. This design provides a feasible guideline for the efficient synthesis of similar shell‐sheddable micelles consisting of PHPMA coatings.

中文翻译：

壳可脱落的聚（N-2-羟丙基甲基丙烯酰胺）聚合物胶束对阿霉素的双重敏感性释放

聚乙二醇（PEG）可脱壳的胶束被证明是快速细胞内药物递送的有效工具。然而，一些不利因素，例如潜在的免疫原性和加速的血液清除，可能伴随着传统的PEG可脱落胶束。在这里，准备了一个在主链上包含二硫键的聚（N-2-羟丙基甲基丙烯酰胺）（PHPMA）可脱落的嵌段共聚物，以形成对pH和还原双反应的胶束。嵌段共聚物的最佳合成途径选自三个潜在途径。阿霉素通过酸不稳定的键加载，以实现较高的药物加载量并防止药物过早释放。不出所料制备的可从外壳脱落的胶束比不可从外壳脱落的胶束显示出更快的细胞内药物释放和更令人满意的体外抗癌效果。该设计为有效合成由PHPMA涂层组成的类似可从外壳脱落的胶束提供了可行的指南。

更新日期：2018-05-16

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