Radiosynthesis and micro-SPECT imaging of 99mTc-dendrimer poly(amido)-amine folic acid conjugate

Bioorg Med Chem Lett. 2010 Feb 1;20(3):927-31. doi: 10.1016/j.bmcl.2009.12.075. Epub 2009 Dec 24.

Abstract

Acetylated (Ac) dendrimer poly(amido)-amine (PAMAM) generation 5 (G5) reacted with folic acid (FA), followed by reacting with 2-(p-isothiocyanatobenzyl)-6-methyl-diethylenetria minepentaacetic acid (1B4M DTPA) to form the conjugate of Ac-G5-FA-1B4M DTPA which was further radiolabeled with (99m)Tc. The radiochemical yield is up to 98.9% with excellent in vitro/in vivo stability, rapid blood clearance and certain tumor accumulation which was further confirmed by micro-SPECT imaging study.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Dendrimers / chemical synthesis*
  • Folic Acid / chemical synthesis*
  • Mice
  • Mice, Inbred BALB C
  • Mice, Nude
  • Neoplasms / diagnostic imaging
  • Polyamines / chemical synthesis*
  • Radioisotopes / chemistry
  • Technetium / chemistry*
  • Tomography, Emission-Computed, Single-Photon* / methods

Substances

  • Dendrimers
  • Poly(amidoamine)
  • Polyamines
  • Radioisotopes
  • Technetium
  • Folic Acid