Carbon-based nanomaterials (CNMs) have attracted great attention in biomedical applications such as cancer imaging and therapy. CNMs, which are currently used in a wide range of applications, suffer from drawbacks of toxicity and low biocompatibility. Either noncovalent or covalent functionalization of CNMs with hydrophilic and biocompatible polymers which help to block hydrophobic interactivity between CNMs and cells can greatly increase their biocompatibility by eliminating their probable toxicity towards living organisms. In this report, we present a comparison of both noncovalent and covalent functionalization approaches in order to introduce a biocompatible glycoblock copolymer onto multi-walled carbon nanotubes (CNTs) in order to enhance their potential in therapies. An anticancer drug (doxorubicin, Dox) was conjugated with two different end functionalized poly(1-O-methacryloyl-β-D-fructopyranose-b-(2-methacryloxyethoxy))benzaldehyde glycoblock copolymers, which were synthesized via reversible addition–fragmentation chain transfer (RAFT) polymerization, by either noncovalent or covalent tethering. CNTs were coated separately with the synthesized drug-conjugated glycoblock copolymers and folic acid (FA) to obtain an efficient drug delivery platform for dual-targeting of glucose transporter protein (GLUT5) and folic acid receptors (FR) in breast cancer. A library of synthesized monomers, polymers and prepared glycoblock copolymer coated CNTs (hybrid-CNTs) using both approaches were comprehensively characterized by various techniques. Transmission electron microscopy measurements showed the homogeneous, smooth morphology of the prepared Dox-conjugated glycoblock copolymer coating of CNTs and confocal laser scanning microscopy images displayed successful cellular internalization of hybrid-CNTs in the MCF-7 and MDA-MB-231 human breast cancer cell lines. This research demonstrates the potential of hybrid-CNTs as a biocompatible drug delivery system as well as in vitro use of Dox-conjugated vehicles for dual receptor mediated breast cancer therapy.

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糖聚合物修饰的多壁碳纳米管用于双重靶向乳腺癌治疗

碳基纳米材料（CNM）在生物医学应用（例如癌症成像和治疗）中引起了极大的关注。目前广泛使用的CNM具有毒性和生物相容性低的缺点。CNM的非共价或共价功能化与亲水性和生物相容性聚合物有助于阻止CNM与细胞之间的疏水性相互作用，可以消除它们对生物体的可能毒性，从而大大提高其生物相容性。在本报告中，我们介绍了非共价和共价功能化方法的比较，目的是将生物相容性糖嵌段共聚物引入多壁碳纳米管（CNT），以增强其在治疗中的潜力。抗癌药（阿霉素，ø -methacryloyl-β- d -fructopyranose- b - （2-甲基丙烯酰）氧基）苯甲醛glycoblock共聚物，其合成通过可逆加成-断裂链转移（RAFT）聚合，通过非共价或共价束缚。用合成的药物共轭糖嵌段共聚物和叶酸（FA）分别涂覆CNT，以获得用于乳腺癌中葡萄糖转运蛋白（GLUT5）和叶酸受体（FR）双重靶向的有效药物递送平台。通过两种技术全面表征了使用两种方法合成的单体，聚合物和制备的糖嵌段共聚物涂层的CNT（杂化CNT）的库。透射电子显微镜测量显示均匀，制备的CNT的Dox共轭糖嵌段共聚物涂层的光滑形态和共聚焦激光扫描显微镜图像显示，在MCF-7和MDA-MB-231人乳腺癌细胞系中，成功的杂化CNT细胞内在化。这项研究证明了杂化碳纳米管作为一种生物相容性药物传递系统的潜力以及Dox偶联载体在体外用于双受体介导的乳腺癌治疗。