One Stone Kills Three Birds: Novel Boron-Containing Vesicles for Potential BNCT, Controlled Drug Release, and Diagnostic Imaging
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- 作者：Gaojian Chen ; Jingying Yang ; Gang Lu ; Pi Chu Liu ; Qianjin Chen ; Zuowei Xie ; Chi Wu
- 刊名：Molecular Pharmaceutics
- 出版年：2014
- 出版时间：October 6, 2014
- 年：2014
- 卷：11
- 期：10
- 页码：3291-3299
- 全文大小：405K
- ISSN：1543-8392
文摘
A new conjugate polymer was prepared by an efficient thiol鈥揺ne 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鈥揺ne 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.