Design and preparation of proline, tryptophan and poly-l-lysine functionalized magnetic nanoparticles and their radiolabeling with 131I and 177Lu for potential theranostic use

Int J Pharm. 2022 Nov 25:628:122288. doi: 10.1016/j.ijpharm.2022.122288. Epub 2022 Oct 14.

Abstract

Surface modification of magnetic nanoparticles with poly-l-lysine, proline, and tryptophan was used to design potential theranostic agents for the application in cancer diagnosis and radionuclide-hyperthermia therapy. Characterization of bare and functionalized magnetic nanoparticles was performed in detail. The transparency of the examined magnetic nanoparticles was measured in the non-alternating magnetic field for a complete and better understanding of hyperthermia. For the first time amino acid-functionalized magnetic nanoparticles were labeled with theranostic radionuclides 131I and 177Lu. The specific absorption rate (SAR) procured for poly-l-lysine functionalized magnetic nanoparticles (SAR values of 99.7 W/g at H0 = 15.9 kA/m and resonant frequency of 252 kHz) demonstrated their possible application in magnetic hyperthermia. Poly-l-lysine functionalized magnetic nanoparticles labeled with 177Lu showed the highest radiochemical purity (>99.00 %) and in vitro stability in saline and serum (>98.00 % up to 96 h). The in vivo analysis performed after their intravenous administration in healthy Wistar rats presented good in vivo stability for several days. Encouraging results as well as magnetic and radiochemical properties of 177Lu-PLL-MNPs (80 °C) justify their further testing toward the potential use as theranostic agents for diagnostic and combined radionuclide-hyperthermia therapeutic applications.

Keywords: Amino acid-functionalized magnetic nanoparticles; Biodistribution; Hyperthermia; Laser transmittance; Radiolabeling.

MeSH terms

  • Animals
  • Hyperthermia, Induced* / methods
  • Iodine Radioisotopes
  • Magnetite Nanoparticles* / chemistry
  • Polylysine
  • Precision Medicine
  • Proline
  • Rats
  • Rats, Wistar
  • Tryptophan

Substances

  • Magnetite Nanoparticles
  • Iodine-131
  • Polylysine
  • Tryptophan
  • Proline
  • Iodine Radioisotopes