Department of Neurosurgery, Virginia Commonwealth University, Richmond, VA, USA.
Nanomedicine (Lond). 2011 Apr;6(3):449-58. doi: 10.2217/nnm.10.134.
Glioblastoma multiforme is the most common and most lethal primary brain tumor in humans, with median survival of approximately 1 year. Owing to the ability of glioma cells to aggressively infiltrate normal brain tissue and survive exposure to current adjuvant therapies, there is a great need for specific targeted nanoplatforms capable of delivering both therapeutic and imaging agents directly to invasive tumor cells.
Gadolinium-containing endohedral fullerenes, highly efficient contrast agents for MRI, were functionalized and conjugated with a tumor-specific peptide and assessed for their ability to bind to glioma cells in vitro.
We report the successful conjugation of the carboxyl functionalized metallofullerene Gd(3)N@C(80)(OH)(-26)(CH(2)CH(2)COOH)(-16) to IL-13 peptides and the successful targeting ability towards brain tumor cells that overexpress the IL-13 receptor (IL-13Rα2).
These studies demonstrate that IL-13 peptide-conjugated gadolinium metallofullerenes could serve as a platform to deliver imaging and therapeutic agents to tumor cells.
多形性胶质母细胞瘤是人类最常见和最致命的原发性脑肿瘤，中位生存期约为 1 年。由于神经胶质瘤细胞能够积极浸润正常脑组织并在现有辅助治疗下存活，因此非常需要能够将治疗剂和成像剂直接递送至侵袭性肿瘤细胞的特异性靶向纳米平台。
含钆的笼状富勒烯是 MRI 的高效对比剂，经过功能化和与肿瘤特异性肽偶联，评估其与体外胶质瘤细胞结合的能力。
我们报告了成功地将羧基功能化的金属富勒烯 Gd(3)N@C(80)(OH)(-26)(CH(2)CH(2)COOH)(-16)与 IL-13 肽偶联，并具有针对过度表达 IL-13 受体 (IL-13Rα2) 的脑肿瘤细胞的靶向能力。
这些研究表明，IL-13 肽偶联的钆金属富勒烯可以作为一种平台，将成像和治疗剂递送至肿瘤细胞。
