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用于钆中子俘获治疗的负载二乙烯三胺五乙酸钆的壳聚糖微球

Gadolinium diethylenetriaminopentaacetic acid-loaded chitosan microspheres for gadolinium neutron-capture therapy.

作者信息

Saha Tapan Kumar, Ichikawa Hideki, Fukumori Yoshinobu

机构信息

Department of Chemistry, Jahangirnagar University, Savar, Dhaka 1342, Bangladesh.

出版信息

Carbohydr Res. 2006 Dec 11;341(17):2835-41. doi: 10.1016/j.carres.2006.09.016. Epub 2006 Oct 11.

Abstract

In order to provide a suitable device that would contain water-soluble drugs, highly water-soluble gadolinium diethylenetriaminopentaacetic acid-loaded chitosan microspheres (CMS-Gd-DTPA) were prepared by the emulsion method using glutaraldehyde as a cross-linker and Span 80 as a surfactant for gadolinium neutron-capture therapy of cancer. The gadolinium content and the mass median diameter of CMS-Gd-DTPA were estimated. The size and morphology of the CMS-Gd-DTPA were strongly influenced by the initial applied weight ratio of Gd-DTPA:chitosan. FTIR spectra showed that the electrostatic interaction between chitosan and Gd-DTPA accelerated the formation of gadolinium-enriched chitosan microspheres. Sufficient amounts of glutaraldehyde and Span 80 were necessary for producing discrete CMS-Gd-DTPA. The CMS-Gd-DTPA having a mass median diameter 11.7microm and 11.6% of gadolinium could be used in Gd-NCT following intratumoral injection.

摘要

为了提供一种能够容纳水溶性药物的合适装置,采用乳液法,以戊二醛为交联剂、Span 80为表面活性剂,制备了用于癌症钆中子俘获治疗的高水溶性负载钆二乙烯三胺五乙酸的壳聚糖微球(CMS-Gd-DTPA)。对CMS-Gd-DTPA的钆含量和质量中值直径进行了估算。CMS-Gd-DTPA的尺寸和形态受Gd-DTPA与壳聚糖初始应用重量比的强烈影响。傅里叶变换红外光谱表明,壳聚糖与Gd-DTPA之间的静电相互作用加速了富含钆的壳聚糖微球的形成。制备离散的CMS-Gd-DTPA需要足够量的戊二醛和Span 80。质量中值直径为11.7微米且钆含量为11.6%的CMS-Gd-DTPA可在瘤内注射后用于钆中子俘获治疗。

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