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Structurally simple redox polymersomes for doxorubicin delivery
European Polymer Journal ( IF 5.8 ) Pub Date : 2020-08-01 , DOI: 10.1016/j.eurpolymj.2020.109952
Elena Benito , Lucía Romero-Azogil , Elsa Galbis , M.-Violante de-Paz , M.-Gracia García-Martín

Abstract A simple redox amphiphilic tri-block copolyurethane capable of assembling in the form of polymersome has been easily synthesized. Thus, the hydrophobic core is constituted by a central block containing multiple disulfide linkages, and the hydrophilic segments are formed by poly(ethylene glycol) methyl ether (mPEG2000). The disulfide-containing block was obtained by the reaction of commercial 2,2’-dithiodiethanol and hexamethylene diisocyanate, which was further reacted with the mentioned PEG to afford the tri-block copolymer nominated as mPEG-PDH-mPEG, in above 80% yield. This copolymer self-assembled into polymersomes of size around 130 nm by the water addition/solvent evaporation method. Different systems of doxorubicin/polymer ratios (D/P 0.5 – 3) were prepared and the drug loading (%DL) and encapsulation efficiency (%EE) were studied by visible light absorbance measurements. Systems D/P 2 and 3 showed DL up to 62% and 69%, respectively. Besides that, D/P 1 and 2 presented EE values in the order of 83%. Finally, the release of DOX in the presence of 0.01 M glutathione solutions at 37 °C, was 74.6% and 82% from D/P 3 and D/P 0.5, respectively, after 5 days of incubation. Further studies on other water-soluble drugs for the cancer treatment would be of great interest to demonstrate the high potential of these redox polymeric systems.

中文翻译:

用于多柔比星递送的结构简单的氧化还原聚合物囊泡

摘要 一种能够以聚合物囊泡形式组装的简单氧化还原两亲性三嵌段共聚聚氨酯已被很容易地合成。因此,疏水核由包含多个二硫键的中心嵌段构成,亲水链段由聚(乙二醇)甲基醚(mPEG2000)形成。含二硫化物的嵌段是由市售的 2,2'-二硫二乙醇和六亚甲基二异氰酸酯反应得到的,再与上述 PEG 反应得到三嵌段共聚物,命名为 mPEG-PDH-mPEG,产率超过 80% . 这种共聚物通过加水/溶剂蒸发方法自组装成大小约为 130 nm 的聚合物囊泡。多柔比星/聚合物比率的不同系统 (D/P 0. 5 – 3) 的制备和载药量 (%DL) 和包封率 (%EE) 通过可见光吸光度测量进行研究。系统 D/P 2 和 3 的 DL 分别高达 62% 和 69%。除此之外,D/P 1 和 2 的 EE 值约为 83%。最后,在 0.01 M 谷胱甘肽溶液存在下,在 37°C 下,DOX 的释放量分别为 D/P 3 和 D/P 0.5 的 74.6% 和 82%,孵育 5 天后。对用于癌症治疗的其他水溶性药物的进一步研究将非常有趣,以证明这些氧化还原聚合物系统的巨大潜力。在培养 5 天后,D/P 3 和 D/P 0.5 分别为 74.6% 和 82%。对用于癌症治疗的其他水溶性药物的进一步研究将非常有趣,以证明这些氧化还原聚合物系统的巨大潜力。在培养 5 天后,D/P 3 和 D/P 0.5 分别为 74.6% 和 82%。对用于癌症治疗的其他水溶性药物的进一步研究将非常有趣,以证明这些氧化还原聚合物系统的巨大潜力。
更新日期:2020-08-01
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