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Glycopolymer and Poly(β-amino ester)-Based Amphiphilic Block Copolymer as a Drug Carrier
Biomacromolecules ( IF 5.5 ) Pub Date : 2022-11-01 , DOI: 10.1021/acs.biomac.2c01076 Elif L Sahkulubey Kahveci 1 , Muhammet U Kahveci 2 , Asuman Celebi 3 , Timucin Avsar 3 , Serap Derman 1
Biomacromolecules ( IF 5.5 ) Pub Date : 2022-11-01 , DOI: 10.1021/acs.biomac.2c01076 Elif L Sahkulubey Kahveci 1 , Muhammet U Kahveci 2 , Asuman Celebi 3 , Timucin Avsar 3 , Serap Derman 1
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Glycopolymers are synthetic macromolecules having pendant sugar moieties and widely utilized to target cancer cells. They are usually considered as a hydrophilic segment of amphiphilic block copolymers to fabricate micelles as drug carriers. A novel amphiphilic block copolymer, namely, poly(2-deoxy-2-methacrylamido-d-glucose-co-2-hydroxyethyl methacrylate)-b-poly(β-amino ester) [P(MAG-co-HEMA)-b-PBAE], with active cancer cell targeting potential and pH responsivity was prepared. Tetrazine end functional P(MAG-co-HEMA) and norbornene end functional PBAE blocks were separately synthesized through reversible addition fragmentation chain transfer polymerization and Michael addition-based poly-condensation, respectively, and followed by end-group transformation. Then, inverse electron demand Diels Alder reaction between the tetrazine and the norbornene groups was performed by simply mixing to obtain the amphiphilic block copolymer. After characterization of the block copolymer in terms of chemical structure, pH responsivity, and drug loading/releasing, pH-responsive micelles were obtained with or without doxorubicin (DOX), a model anticancer drug. The micelles exhibited a sharp protonated/deprotonated transition on tertiary amine groups around pH 6.75 and the pH-specific release of DOX below this value. Eventually, the drug delivery potential was evaluated by cytotoxicity assays on both the noncancerous human umbilical vein endothelial cell (HUVEC) cell line and glioblastoma cell line, U87-MG. While the DOX-loaded polymeric micelles were not toxic in noncancerous HUVEC cells, being toxic only to the cancer cells indicates that it is a potential specific cell targeting strategy in the treatment of cancer.
中文翻译：
糖聚合物和聚（β-氨基酯）基两亲性嵌段共聚物作为药物载体
糖聚合物是具有侧链糖部分的合成大分子，广泛用于靶向癌细胞。它们通常被认为是两亲性嵌段共聚物的亲水片段，用于制造作为药物载体的胶束。一种新型两亲性嵌段共聚物，即聚(2-脱氧-2-甲基丙烯酰胺-d-葡萄糖-co -2-甲基丙烯酸羟乙酯) -b-聚(β-氨基酯)[P(MAG- co -HEMA) -b制备了具有活性癌细胞靶向潜力和pH响应性的[-PBAE]。分别通过可逆加成断裂链转移聚合和基于迈克尔加成的缩聚反应分别合成四嗪末端官能化P(MAG- co -HEMA)和降冰片烯末端官能化PBAE嵌段，然后进行端基转化。然后，通过简单混合，进行四嗪与降冰片烯基团之间的逆电子需求狄尔斯阿尔德反应，得到两亲性嵌段共聚物。在对嵌段共聚物的化学结构、pH 响应性和药物负载/释放进行表征后，获得了含有或不含阿霉素 (DOX)（一种模型抗癌药物）的 pH 响应性胶束。在 pH 6.75 左右，胶束在叔胺基团上表现出急剧的质子化/去质子化转变，并且 DOX 的 pH 特异性释放低于该值。最终，通过对非癌性人脐静脉内皮细胞 (HUVEC) 细胞系和胶质母细胞瘤细胞系 U87-MG 进行细胞毒性测定来评估药物输送潜力。 虽然负载 DOX 的聚合物胶束对非癌性 HUVEC 细胞没有毒性，但仅对癌细胞有毒，表明它是治疗癌症的潜在特异性细胞靶向策略。
更新日期：2022-11-01
中文翻译：
糖聚合物和聚（β-氨基酯）基两亲性嵌段共聚物作为药物载体
糖聚合物是具有侧链糖部分的合成大分子，广泛用于靶向癌细胞。它们通常被认为是两亲性嵌段共聚物的亲水片段，用于制造作为药物载体的胶束。一种新型两亲性嵌段共聚物，即聚(2-脱氧-2-甲基丙烯酰胺-d-葡萄糖-co -2-甲基丙烯酸羟乙酯) -b-聚(β-氨基酯)[P(MAG- co -HEMA) -b制备了具有活性癌细胞靶向潜力和pH响应性的[-PBAE]。分别通过可逆加成断裂链转移聚合和基于迈克尔加成的缩聚反应分别合成四嗪末端官能化P(MAG- co -HEMA)和降冰片烯末端官能化PBAE嵌段，然后进行端基转化。然后，通过简单混合，进行四嗪与降冰片烯基团之间的逆电子需求狄尔斯阿尔德反应，得到两亲性嵌段共聚物。在对嵌段共聚物的化学结构、pH 响应性和药物负载/释放进行表征后，获得了含有或不含阿霉素 (DOX)（一种模型抗癌药物）的 pH 响应性胶束。在 pH 6.75 左右，胶束在叔胺基团上表现出急剧的质子化/去质子化转变，并且 DOX 的 pH 特异性释放低于该值。最终，通过对非癌性人脐静脉内皮细胞 (HUVEC) 细胞系和胶质母细胞瘤细胞系 U87-MG 进行细胞毒性测定来评估药物输送潜力。 虽然负载 DOX 的聚合物胶束对非癌性 HUVEC 细胞没有毒性，但仅对癌细胞有毒，表明它是治疗癌症的潜在特异性细胞靶向策略。
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