A novel ABA-type polyethylene glycol (PEG)-b-polyketal (PK)-b-PEG block copolymer was synthesized via click reactions between the monoazido-monomethoxy-PEG and dialkyne terminated aliphatic polyketal with no carboxylic/amide linkages. Formation of the novel block copolymer was confirmed by 1H NMR, GPC, TGA, and DSC studies. The formed copolymer has shown faster degradation at acidic pH. Self-assembly of this block copolymer (average size 6.2 nm) was assessed by fluorescence study using pyrene as a probe. Doxorubicin loaded block copolymeric micelles (69.9 nm) have shown pH dependent elevated drug release at pH 6.4, indicating its potential as a pH responsive nano-carrier for anticancer therapy. The nano-sized copolymer demonstrated tumoricidal activities against the lymphoma of murine and human origin with significant levels of growth inhibition and apoptosis. Therapy with doxorubicin loaded copolymer reduced the tumor size and augmented the life span of the tumor bearing animals with improved histopathological parameters, compared with the untreated control.

中文翻译：

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阿霉素负载的pH响应性可生物降解的ABA型两亲性PEG-b-脂族聚缩酮-b-PEG嵌段共聚物，可用于治疗侵袭性鼠淋巴瘤。

通过单叠氮基-单甲氧基-PEG和二烷基封端的无羧基/酰胺键的脂肪族聚缩酮之间的点击反应，合成了一种新型的ABA型聚乙二醇（PEG）-b-聚缩酮（PK）-b-PEG嵌段共聚物。通过1 H NMR，GPC，TGA和DSC研究证实了新型嵌段共聚物的形成。所形成的共聚物在酸性pH下显示出更快的降解。使用block作为探针，通过荧光研究评估了该嵌段共聚物的自组装（平均粒径为6.2 nm）。载有阿霉素的嵌段共聚物胶束（69.9 nm）在pH 6.4时显示出pH依赖性药物释放升高，表明其作为抗癌治疗的pH响应性纳米载体的潜力。纳米级共聚物表现出对鼠类和人类来源淋巴瘤的杀伤活性，并具有显着水平的生长抑制和细胞凋亡。与未治疗的对照组相比，用阿霉素负载的共聚物进行的治疗可减少肿瘤的大小，并通过改善组织病理学参数来延长荷瘤动物的寿命。