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Fabrication of Conjugated Amphiphilic Triblock Copolymer for Drug Delivery and Fluorescence Cell Imaging
ACS Biomaterials Science & Engineering ( IF 5.8 ) Pub Date : 2018-01-23 00:00:00 , DOI: 10.1021/acsbiomaterials.7b00991
Xuezhi Zhao 1 , Kaicheng Deng 1 , Fangjun Liu 1 , Xiaolong Zhang 1 , Huiru Yang 1 , Jinlei Peng 1 , Zengkui Liu 1 , Liwei Ma 1 , Baoyan Wang 1 , Hua Wei 1
Affiliation  

An elegant integration of light-emitting segments into the structure of polymeric delivery systems endows the resulting self-assembled nanovehicles with the diagnostic ability toward an enhanced therapeutic efficiency. A variety of polyfluorene (PF)-based binary delivery systems were designed and developed successfully, but PF-based ternary formulations remain rarely explored, likely due to the synthetic challenge. To develop a universal synthesis strategy toward linear conjugated amphiphilic triblock copolymer for cancer theranostics, herein we focused on the functionalization of the PF terminus for further chain extension and prepared well-defined PF-based amphiphilic triblock copolymers, PF-b-poly(ε-caprolactone)-b-poly(oligo(ethylene glycol) monomethyl ether methacrylate) (PF-b-PCL-b-POEGMA), by integrated state-of-the-art polymer chemistry techniques, including Suzuki reaction, ring-opening polymerization, atom transfer radical polymerization, and click coupling. The resulting conjugated amphiphilic triblock copolymers can self-assembe into core–shell-corona (CSC) micelles with PF block constructing the inner hydrophobic core for fluorescent tracking, PCL segment forming the hydrophobic middle shell for drug encapsulation, and POEGMA moiety building the hydrophilic outer corona for particulate stabilization. Interestingly, the CSC micelles with hydrophobic PCL middle layer show a greater drug loading capacity as well as a higher fluorescence quantum yield (Φ) relative to the core–shell micelles self-assembled from the control of PF-b-POEGMA diblock copolymers without PCL sequence due to having more hydrophobic spaces and better separation of PF sequence provided simultaneously by the PCL central block. The efficient cellular uptake of the anticancer drug doxorubicin-loaded CSC micelles together with the in vitro cytotoxicity against the HeLa cells makes the conjugated amphiphilic triblock copolymers developed herein a promising platform for simultaneous cell image and drug delivery, thus offering great potential for cancer theranostics.

中文翻译:

共轭两亲性三嵌段共聚物的制备,用于药物递送和荧光细胞成像

发光段与聚合物输送系统结构的完美结合使所得的自组装纳米车辆具有提高治疗效率的诊断能力。成功设计和开发了多种基于聚芴(PF)的二元传递系统,但由于合成挑战,基于PF的三元配方仍然很少探索。为了开发针对癌症治疗学的线性共轭两亲三嵌段共聚物的通用合成策略,本文我们集中于PF末端的功能化以进一步扩链,并制备了定义明确的基于PF的两亲三嵌段共聚物PF- b -poly(ε-己内酯)-b-聚(低聚(乙二醇)单甲基醚甲基丙烯酸甲酯)(PF-b -PCL- b -POEGMA),通过集成的最新聚合物化学技术,包括Suzuki反应,开环聚合,原子转移自由基聚合和点击偶联。生成的共轭两亲三嵌段共聚物可以自组装成核-壳-电晕(CSC)胶束,其中PF嵌段构成了用于荧光跟踪的内部疏水核,PCL段形成了用于药物封装的疏水中间壳,而POEGMA部分则构建了亲水性外部用于微粒稳定的电晕。有趣的是,相对于由PF- b控制而自组装的核-壳胶束,具有疏水性PCL中间层的CSC胶束显示出更大的载药量以及更高的荧光量子产率(Φ)。-没有PCL序列的-POEGMA二嵌段共聚物,因为具有更多的疏水空间和由PCL中心嵌段同时提供的PF序列更好的分离。负载抗癌药阿霉素的CSC胶束的有效细胞摄取以及对HeLa细胞的体外细胞毒性,使得本文开发的共轭两亲三嵌段共聚物成为同时进行细胞成像和药物递送的有希望的平台,因此为癌症治疗学提供了巨大潜力。
更新日期:2018-01-23
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