STTR Phase I: Novel Water-Soluble TNT Metallofullerene Derivatives for Imaging Applications

这个小企业技术转让（STTR）第一阶段项目提出了功能化TNT-金属富勒烯与高度水溶性，空间稳定的配体，并评估这些材料作为一般的MRI（磁共振成像）造影剂。典型的内嵌金属富勒烯的产率极低，并且在空气中不稳定。相比之下，研究人员开发的三金属氮化物模板（TNT）工艺允许生产一类新的非常稳定的内嵌金属富勒烯，其数量足以进行研究。诊断和治疗领域的生物医学应用提供了利用这些材料的近期机会，因为这些应用所需的数量相对较小，并且这些纳米材料提供了优于当前系统的独特优势。TNT工艺允许封装1-3个顺磁性镧系元素，将金属与身体隔离。初步数据表明，羟基化，含钆TNT-金属富勒烯增加周围的水分子的质子弛豫速率显着超过目前使用的钆螯合物。然而，典型的羟基化富勒烯的聚集阻止了它们的最大效率和效用。添加大的，高度可溶的配体，预计将促进增强水溶性，阻止聚集，并提供一个更大的增强比目前的钆MRI造影剂。该项目的商业应用是在生物医学成像领域。

This Small Business Technology Transfer (STTR) Phase I Project proposes to functionalize TNT-metallofullerenes with highly water-soluble, steric-stabilizing ligands and to evaluate these materials as general MRI(Magnetic Resonance Imaging) contrast agents. Classical endohedral metallofullerenes are produced in exceedingly low yields and are unstable in air. In contrast, the development of trimetallic-nitride-template (TNT) process by the investigators has allowed the production of a new class of extremely stable endohedral metallofullerenes in sufficient research quantities. Biomedical applications in diagnostic and therapeutic areas offer a near-term opportunity to utilize these materials because the quantities required for such applications are relatively small, and these nanomaterials offer unique advantages over current systems. The TNT process allows the encapsulation of 1-3 paramagnetic lanthanides, isolating the metals from the body. Preliminary data indicates that hydroxylated, gadolinium-containing TNT-metallofullerenes increase the proton relaxation rate of surrounding water molecules significantly over currently used gadolinium chelates. However, aggregation of typical hydroxylated fullerenes prevents their maximum efficiency and utility. Addition of large, highly soluble ligands is expected to promote enhanced water solubility, deter aggregation, and deliver an even larger enhancement over current gadolinium MRI contrast agents.The commercial applications of this project are in the area of Biomedical Imaging.