Chen Gaojian, Yang Jingying, Lu Gang, Liu Pi Chu, Chen Qianjin, Xie Zuowei, Wu Chi
Department of Chemistry, The Chinese University of Hong Kong , Shatin, New Territories, Hong Kong.
Mol Pharm. 2014 Oct 6;11(10):3291-9. doi: 10.1021/mp400641u. Epub 2014 Feb 20.
A new conjugate polymer was prepared by an efficient thiol-ene coupling of one carborane with a linear PEG chain (Mn = 2,000 g/mol), and each carborane was further labeled with a fluorescence rhodamine dye. Such a novel polymer can associate in water to form narrowly distributed spherical vesicles, which were characterized using a range of methods, including laser light scattering, confocal laser scanning microscopy, and TEM. The vesicular structure is potentially multifunctional in biomedical applications, namely, serving as a boron neutron capture therapy (BNCT) agent, a hydrophilic drug carrier, and a diagnostic imaging fluorescent probe. As expected, either cleaving the thiol-ene linked PEO chain by esterase or destroying carborane by neutron irradiation results in a dismantlement of such a vesicle structure to release its encapsulated drugs. Its potential biomedical applications have been evaluated in vitro and in vivo. Our preliminary results reveal that these small vesicles can be quickly taken up by cells and have an enhanced stability in the bloodstream so that their targeting to specific cancer cells becomes feasible.
通过一种碳硼烷与线性聚乙二醇链（Mn = 2000 g/mol）的高效硫醇-烯偶联反应制备了一种新型共轭聚合物，并且每个碳硼烷都进一步用荧光罗丹明染料进行了标记。这种新型聚合物在水中能够缔合形成分布狭窄的球形囊泡，使用一系列方法对其进行了表征，包括激光光散射、共聚焦激光扫描显微镜和透射电子显微镜。这种囊泡结构在生物医学应用中具有潜在的多功能性，即作为硼中子俘获疗法（BNCT）试剂、亲水性药物载体和诊断成像荧光探针。正如预期的那样，通过酯酶裂解硫醇-烯连接的聚环氧乙烷链或通过中子辐照破坏碳硼烷都会导致这种囊泡结构解体，从而释放其包裹的药物。已经在体外和体内对其潜在的生物医学应用进行了评估。我们的初步结果表明，这些小囊泡能够被细胞快速摄取，并且在血液中具有更高的稳定性，因此它们靶向特定癌细胞变得可行。
