Conjugation of Functionalized Gadolinium Metallofullerenes with IL-13 Peptides for Targeting and Imaging Glial Tumors

Abstract

These studies demonstrate that IL-13 peptide-conjugated gadolinium metallofullerenes could serve as a platform to deliver imaging and therapeutic agents to tumor cells.

Metallofullerenes: A New Class of MRI Agents and More?

“…If this agent were carrying a b-emitter for brachytherapy (e.g., 177 Lu or 90 Y) it could potentially provide pertinent data on tumor response to therapy through longitudinal imaging without further contrast administrations. A basic example of this can be seen in Figure 1D showing MRI images 30 min (Figure 1Di) and 24 h (Figure 1Dii) post intratumoral infusion by CED [45]. The prolonged retention of the functionalized metallofullerenes and their ability to enhance the MRI contrast 7 days following live rat brain infusion has also been demonstrated [32].…”

“…This conjugate is depicted in Figure 2C. In these studies, metallo fullerenes conjugated with an IL-13 receptor targeting peptide showed increased affinity for tumor cells that correlated with the expression level of the receptor [45]. While further studies will be required to show the benefit of such targeting for IL-13-targeting peptide 177 Lu chelate for brachytherapy 124 I for PET detection future science group therapeutic treatments, one could speculate that the targeting should increase tumor retention, which is an important parameter in delivering interstitial brachytherapy with a radioisotope.…”

“…Metallofullerenes have become employable in a multitude of medical fields owing to their cagelike structure and diverse material properties that result from encapsulating various metals [3,13,41,42] or decorating the fullerene surface [43,44] with targeting [42,45], diagnostic [46,47] or biofunctional ligands [26,28]. As mentioned earlier, the vision of nanomedicine has fueled further fullerene developments [48,49], primarily owing to their versatile functionality embodied in a single nanoplatform.…”

“…The ability to target particular receptors that are overexpressed in tumors may enhance tumor imaging or increase the delivery of a drug payload to the tumor. In either case, the metallofullerene is capable of being functionalized with targeting ligands [42,45]. This conjugate is depicted in Figure 2C.…”

Neurological disorders and therapeutics targeted to surmount the blood–brain barrier

“…158 Further, conjugation of interleukin-13 peptides with the nanoparticle surface could enhance targeted delivery towards glioma cells, which overexpress the interleukin-13 receptor. 159 Similarly, PEG-PLGA nanoparticles covalently modified with Pep TGN (a 12-amino acid peptide) showed enhanced brain penetration along with reduced accumulation in the liver and spleen in vivo. The significance of this study was that brain-targeted delivery of Pep TGN has never been reported before.…”