MAGNETIC TARGETING OF RADIOACTIVE MICROPARTICLES

放射性微粒的磁靶向

• 批准号: 6209884
• 负责人: Gilles H TAPOLSKY
• 金额: $ 9.96万
• 依托单位: FERX, INC.
• 依托单位国家: 美国
• 财政年份: 2000
• 资助国家: 美国
• 起止时间: 2000-09-25 至 2001-08-31
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/6209884
• 关键词: carbon; drug delivery systems; iron; laboratory rat; magnetism; microcapsule; neoplasm /cancer radionuclide therapy; nonhuman therapy evaluation; radiopharmacology; radiotracer; swine; technology /technique development

The ability to deliver high doses of radiation to a tumor without significant damage to surrounding tissue would be a significant advancement in the radiation therapy of solid tumors. FeRx proposes to develop a convenient and safe regimen based on magnetic targeted delivery of radionuclides. Magnetic Targeted Carriers (MTCs) are 0.5 to 1.5 micron microparticles, composed of metallic iron and activated carbon. Using a small externally positioned magnet, MTCs are effectively targeted to a tumor where they are trapped. By irreversibly binding 188Re, a beta emitter radionuclide, to the activated carbon of the MTCs, tumor cells could be safely and effectively irradiated. The combination of a proven targeting technology with an effective radionuclide will lead to a product able to treat a wide variety of tumors in many different organs, with maximal radiation delivered to the tumor and minimal exposure to surrounding tissue. In this proposal we will investigate the feasibility of this project and we plan: 1) to develop and characterize radiolabeled MTCs for their labeling efficiency and labeling stability profile, 2) to evaluate the efficacy of their localization in a rat tumor model, and 3) to evaluate their biodistribution in a normal swine model. PROPOSED COMMERCIAL APPLICATION: Cancer remains one of the leading causes of death in developed countries. While therapies are overall more effective, there is still a tremendous need for less toxic and more effective treatments. The product FeRx proposes to develop would fulfill this need. It would also have a broad range of indications, such as pancreatic, liver, and lung cancers. Commercial opportunities would be very significant. In the lung cancer alone, there was an estimated 171,600 new cases in 1999.

向肿瘤递送高剂量辐射而不显著损伤周围组织的能力将是实体肿瘤的辐射治疗的显著进步。FeRx建议开发一种基于放射性核素磁靶向递送的方便安全的方案。磁性靶向载体（MTC）是由金属铁和活性炭组成的0.5至1.5微米的微粒。使用一个小的外部定位的磁铁，MTCs有效地靶向肿瘤，在那里他们被困。通过将β放射性核素188 Re不可逆地结合到MTCs的活性炭上，可以安全有效地照射肿瘤细胞。将经过验证的靶向技术与有效的放射性核素相结合，将产生一种能够治疗许多不同器官中各种肿瘤的产品，最大限度地向肿瘤提供辐射，并将对周围组织的暴露降至最低。在本提案中，我们将研究该项目的可行性，我们计划：1）开发和表征放射性标记的MTC的标记效率和标记稳定性特征，2）评价其在大鼠肿瘤模型中定位的有效性，3）评价其在正常猪模型中的生物分布。建议的商业应用：癌症仍然是发达国家的主要死亡原因之一。虽然治疗总体上更有效，但仍然需要更少毒性和更有效的治疗方法。FeRx计划开发的产品将满足这一需求。它也有广泛的适应症，如胰腺癌，肝癌和肺癌。商业机会将非常重要。仅肺癌一项，1999年估计就有171 600个新病例。